Month: November 2022

On June 30, 2011, Badiger, Sangamesh; Behnke, Dirk; Betschart, Claudia; Chaudhari, Vinod; Cotesta, Simona; Hinrichs, Juergen Hans-Hermann; Ofner, Silvio; Pandit, Chetan published a patent.Quality Control of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Preparation of diaza-spiro[5.5]undecanes as orexin receptor antagonists. And the patent contained the following:

The title compounds I [A = (un)substituted 8-10 membered fused bicyclic aromatic ring system which may contain from 1-4 heteroatoms selected from N, O and S, wherein the ring system may contain not more than 2 O atoms and not more than 2 S atoms; or A = (un)substituted 5-6 membered monocyclic aromatic ring system which may contain 1-4 heteroatoms selected from N, O and S, wherein the ring system may contain not more than 2 O atoms and not more than 2 S atoms; m = 0-6; n = 0-6; R1, R2 = halo, alkyl, haloalkyl, etc.; X1 = C(O) and X2 = N(LB); or X1 = N(LB) and X2 = C(O); L = C(R7)2; R7 = H, alkyl, haloalkyl, etc.; B = (un)substituted 5-10 membered monocyclic or fused polycyclic aromatic ring system which may contain from 1-4 heteroatoms selected from N, O and S, wherein the ring system may contain not more than 2 O atoms and not more than 2 S atoms], were prepared E.g., a multi-step synthesis of II, starting from indole-3-carboxaldehyde, was described. Exemplified compounds I were tested for inhibition of orexin-1 and orexin-2 receptors binding (data provided). Pharmaceutical compositions comprising the compound I, alone or in combination with other therapeutic agent, were also disclosed. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Quality Control of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

The Article related to diazaspiroundecane preparation orexin receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On June 30, 2022, El-Essawy, Farag A.; Ali, Noora T. G.; Boshta, Nader M. published an article.Application In Synthesis of 3-Acetyldihydrofuran-2(3H)-one The title of the article was Synthesis and Anti-HIV Activity of Poly-Heterocyclic Compounds Containing Quinoline Moiety. And the article contained the following:

A novel series of poly-heterocyclic compounds containing quinoline as antiviral agents against HIV was designed and synthesized. Structures of these novel derivatives was confirmed by IR, NMR, and EI-MS spectra. Most of the products was tested for their HIV inhibitory activity and characterized by high to moderate activity. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Application In Synthesis of 3-Acetyldihydrofuran-2(3H)-one

The Article related to pyrrolo pyrimidopyrazolo quinolinone preparation antiviral agent, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.Application In Synthesis of 3-Acetyldihydrofuran-2(3H)-one

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On March 26, 2015, Marcin, Lawrence R.; Higgins, Mendi A.; Bronson, Joanne J.; Zusi, F. Christopher; Macor, John E.; Ding, Min published a patent.Application In Synthesis of Methyl 2-(2,6-difluorophenyl)acetate The title of the patent was Preparation of triazolopyridine ether derivatives useful in treatment of neurological and psychiatric disorders. And the patent contained the following:

The invention relates to compounds of formula I and their preparation, as modulators of the mGluR2 receptor potentially useful for the treatment of various disorders of the central nervous system including neurol. and psychiatric disorders. Compounds of formula I are claimed, in which R1 is H, CN, halo, (halo)alkyl, etc.; R2 is (halo)alkyl, (cycloalkyl)alkyl, etc.; R3 is Ar1 and OAr1; Ar1 is (un)substituted Ph, pyridinyl, pyrimidinyl, etc.; Y is bond and (un)substituted C3-6 cycloalkyl; Z is bond and (un)substituted C1-3 alkyl; provided that when Y and Z are bonds, R3 is Ar1; or pharmaceutically acceptable salts thereof. Example compound II was prepared by cyclocondensation of 2-hydrazinyl-4-((1-phenylcyclohexyl)methoxy)-3-(trifluoromethyl)pyridine with 2-cyclopropylacetyl chloride to afford 2-cyclopropyl-N’-(4-((1-phenylcyclohexyl)methoxy)-3-(trifluoromethyl)pyridin-2-yl)acetohydrazide, which underwent cyclization with Burgess reagent to yield II. Invention compounds were evaluated for their human mGluR2 inhibitory activity. From the assay, it was determined that II exhibited EC50 value of 1.8 nM. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Application In Synthesis of Methyl 2-(2,6-difluorophenyl)acetate

The Article related to triazolopyridine ether preparation treatment cns neurol psychiatric disorder, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.Application In Synthesis of Methyl 2-(2,6-difluorophenyl)acetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 29, 1998, Duggan, Mark E.; Egbertson, Melissa S.; Hartman, George D.; Young, Steven D.; Ihle, Nathan C. published a patent.Safety of tert-Butyl (4-hydroxy-2-nitrophenyl)carbamate The title of the patent was Preparation of 4-[(4-piperazinobeznoyl)amino]phenyl(oxy)alkanoates as fibrinogen receptor antagonists. And the patent contained the following:

XYZAB [I; A = (un)substituted (hetero)arylene; B = O(CH2)mCO2R9, (CH2)nCO2R9, CHR8(CH2)pCO2R9, OCHR8(CH2)pCO2R9; R8 = H, OH, alkyl, alkoxy, aryl, etc.; R9 = H, (ar)alkyl, aryl, acylalkyl, etc.; X = (un)substituted heterocyclyl or -heteroaryl; Y = (un)substituted heterocyclylene or -(hetero)arylene; Z = bond, NH, CONH, CO, CH2CH2, etc.; m = 1-3; n,p = 0-3] were prepared Thus, 4-(H2N)C6H4CO2Me was cyclocondensed with HN(CH2CH2Cl)2 and the N-protected and saponified product amidated by 4-BrC6H4NH2 to give the bromobenzanilide which was condensed with CH2:CHCO2Me and the product converted in 3 addnl. steps to 4-RC6H4CONHC6H4(CH2CH2CO2H)-4 (R = piperazino). Data for biol. activity of I were given. The experimental process involved the reaction of tert-Butyl (4-hydroxy-2-nitrophenyl)carbamate(cas: 201811-20-3).Safety of tert-Butyl (4-hydroxy-2-nitrophenyl)carbamate

The Article related to piperazinobeznoylaminophenylalkanoate preparation fibrinogen receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of tert-Butyl (4-hydroxy-2-nitrophenyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On July 17, 2020, Qian, Shengyou; Pu, Xingwen; Chang, Guanjun; Huang, Ying; Yang, Yudong published an article.SDS of cas: 141940-37-6 The title of the article was Rh(III)-catalyzed oxidative C-H activation/domino annulation of anilines with 1,3-diynes: a rapid access to blue-emitting tricyclic N,O-heteroaromatics. And the article contained the following:

Disclosed herein is a rhodium-catalyzed oxidative C-H activation/domino annulation of N-Boc-anilines with 1,3-diynes for the construction of tricyclic N,O-heteroaromatics This reaction features easily available substrates, mild reaction conditions, high regioselectivity, mono/diannulation selectivity, and intra/intermol. annulation selectivity. Moreover, this synthetic protocol enables the rapid assembly of a library of blue-emitting mols. with high quantum yields, among of which two fluorophores with pure blue-emission in toluene are discovered. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).SDS of cas: 141940-37-6

The Article related to rhodium catalysis oxidative anilines diyne tricyclic blue emitting heteroaromatic, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Other Dyes and Pigments and other aspects.SDS of cas: 141940-37-6

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On September 30, 2021, Choi, Si Woo; Ryu, Soo Hee; Ryu, Ji Hoon; Son, San Ha; Lee, Hwa Jin; Kim, Seong Hoon; Nam, Boas; Min, Im Suk; Ryu, Hye Guk; Kang, Keum Young published a patent.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Preparation of pyrimidodiazepine derivatives as PLK1 selective degradation inducers for the treatment and prevention of PLK1-related diseases. And the patent contained the following:

The invention relates to preparation of pyrimidodiazepines that induce selective polo-like kinase 1 (PLK1) degradation Specifically, the invention provides a bifunctional compound in which a PLK1 binding moiety and an E3 ubiquitin ligase-binding moiety are linked by a chem. linker. The example compound I was prepared via 6-steps synthesis using 4-bromobutanoic acid as starting material (procedure given). The compounds of the invention may be effectively utilized in prevention and treatment of PLK1-related diseases. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to pyrimidodiazepine preparation plk1 degradation inducer disease treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On September 15, 2010, Wu, Yusheng; Zou, Dapeng; Li, Jingya; Guo, Ruiyun; Qin, Lijin; Cui, Hongmeng; Cui, Xiuling published a patent.COA of Formula: C12H14F3NO2 The title of the patent was Catalysis system for preparation of N-Boc arylamines. And the patent contained the following:

The catalysis system consists of Pd acetate, phosphine ligand XPhos and Cs carbonate at a mol. ratio 1:3:45-50. The preparation comprises adding Pd acetate, phosphine ligand XPhos, Cs carbonate, tertbutyl amino formate, aryl halide, and anhydrous dioxane at a mol. ratio 0.03:0.09:1.35-1.50:1.2:1:90-95 in a dry reactor, stirring, reacting at 100°C for 1.5-24 h in inert gas (nitrogen) protection, adding water after finishing reaction, extracting with Et acetate, combining organic phases, drying the combined organic phases, concentrating, and purifying. The aryl halide is aryl chloride, aryl bromide, heterogeneous aryl chloride or heterogeneous aryl bromide. The catalysis system can be used for preparation of N-Boc-arylamine compounds The invention has the advantages of mild condition, easy operation, simple post treatment, high yield, less environment pollution, etc.. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).COA of Formula: C12H14F3NO2

The Article related to arylamine butoxycarbonyl preparation aryl halide carbamate coupling catalyst palladium, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.COA of Formula: C12H14F3NO2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On November 12, 2009, Chesworth, Richard; Shapiro, Gideon; Chantigny, Yves; Mancuso, John; Deziel, Robert published a patent.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate The title of the patent was Preparation of azabicyclo[2.2.1]heptan-2-yl compounds as HDAC inhibitors and therapeutic uses thereof. And the patent contained the following:

Inhibitors of histone deacetylase of general formula I (wherein R4 is H, C1-C6alkyl, C2-C6 alkenyl, etc.; each A is N, N-oxide, -CH=, and -C(R4)=; Z is -N(R1)OR2 or H; L is a covalent bond or -C0-C3alkyl-N(OR2)-; G2 is C or N; U2 is a covalent bond, -C1-C6alkyl, C3-C6cycloalkyl, etc.; R200, R201, R202 and R203 are independently H, C1-C6alkyl, aryl, etc.; B3 is H, aryl, heteroaryl, etc.; R1 and R2 are independently H, C1-C6alkyl, aryl, etc.) are described together with methods for treating various disorders with such compounds Such disorders include Huntington’s disease, dentatorubralpallidoluysian atrophy, spinal and bulbar muscular atrophy, and spinocerebellar ataxias. Synthetic procedures for preparing I are exemplified, but no biol. data is given. Example compound II was prepared in a 5-step synthesis that involved reaction of intermediate (1S,4S)-2-benzhydryl-2,5-diazabicyclo[2.2.1]heptane 2HCl with Et 2-(methylsulfonyl)pyrimidine-5-carboxylate and reaction of the intermediate formed with hydroxylamine. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

The Article related to azabicycloheptanyl compound preparation hdac inhibitor nervous system disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On August 13, 2020, Hwang, Jong Yeon; Ha, Jae Du; Cho, Sung Yun; Kim, Pilho; Yun, Chang Soo; Kim, Hyun Jin; Park, Sung Goo; Park, Byoung Chul; Kim, Jeong Hoon; Kim, Sunhong published a patent.SDS of cas: 882518-89-0 The title of the patent was Preparation of target protein EED degradation-inducing degraducer for preventing or treating diseases related to EED, EZH2, or PRC2. And the patent contained the following:

The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound ULB-L-PTM [PTM = EED targeting mols.; L = single bond, chem. linker; ULB = cereblon, MDM2, cIAP, VHL E3 ubiquitin ligase binder] is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).SDS of cas: 882518-89-0

The Article related to preparation target protein eed degradation inducing degraducer, eed ezh2 prc2 disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 882518-89-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 9, 2020, Zhu, Zixi; Glinkerman, Christopher M.; Boger, Dale L. published an article.Recommanded Product: 707-07-3 The title of the article was Selective N1/N4 1,4-Cycloaddition of 1,2,4,5-Tetrazines Enabled by Solvent Hydrogen Bonding. And the article contained the following:

An unprecedented 1,4-cycloaddition (vs 3,6-cycloaddition) of 1,2,4,5-tetrazines is described with preformed or in situ generated aryl-conjugated enamines promoted by the solvent hydrogen bonding of hexafluoroisopropanol (HFIP) that is conducted under mild reaction conditions (0.1 M HFIP, 25°C, 12 h). The reaction constitutes a formal [4 + 2] cycloaddition across the two nitrogen atoms (N1/N4) of the 1,2,4,5-tetrazine followed by a formal retro [4 + 2] cycloaddition loss of a nitrile and aromatization to generate a 1,2,4-triazine derivative The factors that impact the remarkable change in the reaction mode, optimization of reaction parameters, the scope and simplification of its implementation through in situ enamine generation from aldehydes and ketones, the reaction scope for 3,6-bis(thiomethyl)-1,2,4,5-tetrazine, a survey of participating 1,2,4,5-tetrazines, and key mechanistic insights into this reaction are detailed. Given its simplicity and breath, the study establishes a novel method for the simple and efficient one-step synthesis of 1,2,4-triazines under mild conditions from readily accessible starting materials. Whereas alternative protic solvents (e.g., MeOH vs HFIP) provide products of the conventional 3,6-cycloaddition, the enhanced hydrogen bonding capability of HFIP uniquely results in promotion of the unprecedented formal 1,4-cycloaddition As such, the studies represent an example of not just an enhancement in the rate or efficiency of a heterocyclic azadiene cycloaddition by hydrogen bonding catalysis but also the first to alter the mode (N1/N4 vs C3/C6) of cycloaddition The experimental process involved the reaction of (Trimethoxymethyl)benzene(cas: 707-07-3).Recommanded Product: 707-07-3

The Article related to tetrazine aldehyde pyrrolidine hfip cycloaddition, ketone tetrazine pyrrolidine hfip cycloaddition, triazine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.Recommanded Product: 707-07-3

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics