Tag: 200-300

On June 23, 2021, Nicolaou, K. C.; Pan, Saiyong; Shelke, Yogesh; Das, Dipendu; Ye, Qiuji; Lu, Yong; Sau, Susanta; Bao, Ruiyang; Rigol, Stephan published an article.Formula: C12H16O7 The title of the article was A Reverse Approach to the Total Synthesis of Halichondrin B. And the article contained the following:

A new strategy is described for the total synthesis of halichondrin B featuring reversal of the sequential construction of a number of its cyclic ethers from the classical approach by instead forming C-O bonds first followed by C-C bond formation. Employing the Nicholas reaction to generate linear ethers as precursors for the total synthesis of halichondrin B and other members of the halichondrin and eribulin families of compounds, this novel approach provides new opportunities for the development of improved syntheses of these complex and valuable compounds In this Article, we report the syntheses of defined fragments I (I), MN (II), EFG (III), and A (IV). Fragments I and MN were then coupled and elaborated to advanced intermediate IJKLMN, which was joined with fragment EFG to afford, after appropriate elaboration and macrolactonization, the more advanced polycyclic intermediate EFGHIJKLMN. Elaboration of the latter and coupling with fragment A followed by further functionalization completed the total synthesis of halichondrin B through a short and convergent pathway. The experimental process involved the reaction of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate(cas: 2873-29-2).Formula: C12H16O7

The Article related to diastereoselective horner wadsworth emmons nozaki hiyama kishi nicholas etherification, halichondrin b total synthesis, Biomolecules and Their Synthetic Analogs: Others, Including Purines, Pyrimidine Nucleic Acid Bases, Flavins, Lignans and other aspects.Formula: C12H16O7

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

On December 4, 2020, Yang, Feiyan; Ding, Decai; Wang, Chuan published an article.Safety of Phenyl Salicylate The title of the article was Nickel-Catalyzed Directed Cross-Electrophile Coupling of Phenolic Esters with Alkyl Bromides. And the article contained the following:

Herein, we demonstrate the successful use of robust phenolic esters as an electrophilic acyl source in the reaction with diverse primary and secondary unactivated alkyl bromides. The cleavage of the relatively inert C-O bond is facilitated by the neighboring coordinating hydroxyl or sulfonamide moiety. By circumventing the use of pregenerated organometallics, this method allows efficient preparation of a variety of o-hydroxyl and tosyl-protected o-amino aryl ketones with high compatibility with a wide range of functionalities. The experimental process involved the reaction of Phenyl Salicylate(cas: 118-55-8).Safety of Phenyl Salicylate

The Article related to phenolic ester alkyl bromide nickel catalyst cross electrophile coupling, aryl ketone preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ethers, Sulfides, and The Corresponding Onium Compounds and other aspects.Safety of Phenyl Salicylate

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

On January 30, 2014, Ding, Fa-Xiang; Dong, Shuzhi; Frie, Jessica; Gu, Xin; Jiang, Jinlong; Pasternak, Alexander; Tang, Haifeng; Wu, Zhicai; Yu, Yang; Suzuki, Takao published a patent.Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Preparation of 2,8-diazaspiro[4.5]decan-1-one derivatives as inhibitors of the renal outer medullary potassium channel. And the patent contained the following:

The present invention provides compounds of Formula I [ R1 = H, halo, OH or C1-3 alkoxy; m = 0 or 1; n = 1 or 2; R2 = H, oxo, OH, etc.; R3a = H, oxo, C3-4 cycloalkyl, etc.; R3b = H, or C1-3 alkyl; R4 = H or oxo; R5 = H, halo, (un)substituted C1-3 alkyl, etc.; R6 = H or C1-3 alkyl; R7a = H, or (un)substituted C1-3 alkyl; R7b = H or C1-3 alkyl; R8 = H, halo or C1-3 alkyl; R9 = H, F, OH, etc.; R10 = H, halo, CN, etc.; R11 and R12 = H, CH2OH, CH2OCH3 or C1-3 alkyl optionally substituted with 1- 3 of F; R13 = H, SO2Me, (un)substituted C1-3 alkyl, etc.] and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. Compound II was prepared in a multi-step synthesis and had IC50 of 0.01μM in Thallium Flux assay. Compounds I may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

The Article related to diazaspirodecanone preparation romk inhibitor cardiovascular disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

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

On January 30, 2014, Ding, Fa-Xiang; Dong, Shuzhi; Frie, Jessica; Gu, Xin; Jiang, Jinlong; Pasternak, Alexander; Tang, Haifeng; Wu, Zhicai; Yu, Yang; Suzuki, Takao published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of 2,8-diazaspiro[4.5]decan-1-one derivatives as inhibitors of the renal outer medullary potassium channel. And the patent contained the following:

The present invention provides compounds of Formula I [ R1 = H, halo, OH or C1-3 alkoxy; m = 0 or 1; n = 1 or 2; R2 = H, oxo, OH, etc.; R3a = H, oxo, C3-4 cycloalkyl, etc.; R3b = H, or C1-3 alkyl; R4 = H or oxo; R5 = H, halo, (un)substituted C1-3 alkyl, etc.; R6 = H or C1-3 alkyl; R7 = H, or (un)substituted C1-3 alkyl; R7b = H or C1-3 alkyl; R8 = H, halo or C1-3 alkyl; R9 = H, F, OH, etc.; R10 = H, halo, CN, etc.; R11 and R12 = H, CH2OH, CH2OCH3 or C1-3 alkyl optionally substituted with 1- 3 of F; R13 = H, SO2Me, (un)substituted C1-3 alkyl, etc.] and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. Compound II was prepared in a multi-step synthesis and had IC50 of 0.01μM in Thallium Flux assay. Compounds I may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Category: esters-buliding-blocks

The Article related to diazaspirodecanone preparation romk inhibitor cardiovascular disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Category: esters-buliding-blocks

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

On November 13, 2014, Guo, Xialing; Zhu, Zhen published a patent.Product Details of 53838-27-0 The title of the patent was Thienopyridine compounds as tyrosine kinase modulators and their preparation. And the patent contained the following:

The invention is directed to compounds of formula I that are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. Compounds of formula I wherein X is NH and derivatives O, and SO0-3; n is 0 – 3; m is 0 – 2; R1 is H, halo, C1-8 alkyl, etc.; R2 is H, alkoxy, alkoxyalkoxy, alkyl, etc.; R3 is (un)substituted C1-5 alkyl, (un)branched C1-5 haloalkyl, C1-5 alkoxy, etc.; R4 is (un)substituted alkoxy, alkoxyalkyl, alkoxycarbonyl, etc.; Y is (CH2)0-3O(CH2)0-3, (CH2)0-4NH(CH2)0-3 and derivatives; (CH2)0-3CO(CH2)0-3, etc.; A and B are independently Ph, naphthyl, 5- to 6-membered heteroaryl, etc.; Z is (CH2)0-1NHCONH(CH)0-1 and derivatives, (CH2)0-1NHCSNH(CH)0-1 and derivatives, (CH2)0-1NHCO and derivatives, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by etherification of Me 7-bromothieno[3,2-b]pyridine-2-carboxylate with 4-aminophenol; the resulting Me 7-(4-aminophenoxy)thieno[3,2-b]pyridine-2-carboxylate underwent addition to 2-fluoro-5-methylphenyl isocyanate to give compound II. All the invention compounds were evaluated for their tyrosine kinase modulatory activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 2 nM to 18 nM toward VEGFR2. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Product Details of 53838-27-0

The Article related to thienopyridine preparation tyrosine kinase modulator, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Product Details of 53838-27-0

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

On November 16, 2018, Reddy, Leleti Rajender; Kotturi, Sharadsrikar; Waman, Yogesh; Ravinder Reddy, Vudem; Patel, Chirag; Kobarne, Ajinath; Kuttappan, Sasikumar published an article.Electric Literature of 141940-37-6 The title of the article was N-Arylation of Carbamates through Photosensitized Nickel Catalysis. And the article contained the following:

A highly efficient method of visible light mediated Ni(II)-catalyzed photoredox N-arylation of Cbz-amines/Boc-amines with aryl electrophiles at room temperature is reported. The methodol. provides a common access to a wide variety of N-aromatic and N-heteroaromatic carbamate products that find use in the synthesis of several biol. active mols. and provides a distinct advantage over traditional palladium-catalyzed Buchwald reaction. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Electric Literature of 141940-37-6

The Article related to carbamate aryl bromide arylation nickel photolysis, arylcarbamate preparation, nickel photosensitized arylation catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.Electric Literature of 141940-37-6

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

On April 25, 2018, Wang, Mingliang; Han, Jilai; Si, Xiaojia; Hu, Yimin; Zhu, Jidong; Sun, Xun published an article.Application In Synthesis of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate The title of the article was Effective approach to ureas through organocatalyzed one-pot process. And the article contained the following:

An efficient approach to N,N’-unsym. substituted ureas ArN(R1)C(O)NH(R2) (R1 = H; R2 = n-Bu, c-hexyl, Bn, etc.; Ar = 4-MeC6H4, 4-MeOC6H4, 4-F3CC6H4, 3-BrC6H4) has been developed through the ammonolysis of N-Boc protected anilines with amines prompted by 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD). Moreover, a convenient protocol for the synthesis of the sym. N,N’-substituted ureas RNHC(O)NHR (R = Ph, 2-ClC6H4, 4-IC6H4, etc.) by one-pot diammonolysis of Boc2O with amines catalyzed by DABCO has also been achieved. With broad substrate scope and mild conditions, these two methods demonstrate practical preparation of both unsym. and sym. ureas. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Application In Synthesis of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate

The Article related to unsym sym urea preparation, amine tert butyl dicarbonate ammonolysis diammonolysis triazabicyclodecene dabco catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.Application In Synthesis of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate

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

On September 17, 2003, Hama, Takuo; Liu, Xiaoxiang; Culkin, Darcy A.; Hartwig, John F. published an article.Formula: C12H15NO4 The title of the article was Palladium-Catalyzed α-Arylation of Esters and Amides under More Neutral Conditions. And the article contained the following:

Two procedures for the α-arylation of carbonyl compounds, under more neutral conditions than those for reactions of aryl halides with alkali metal enolates, are reported. The first procedure rests upon the development of catalysts bearing the hindered pentaphenylferrocenyl di-tert-butylphosphine (Q-phos), and the highly reactive dimeric Pd(I) complex {[P(t-Bu)3]PdBr}2. Zinc enolates, prepared from α-bromo esters and amides, react with aryl bromides to form α-aryl esters, e.g., I (R1 = OCMe3, R2 = H), and amides, e.g., I (R1 = NEt2, R2 = Me), in high yields, and with remarkable functional group tolerance. The second procedure; silyl ketenes II (R3 = t-Bu, R4 = H; R3 = R4 = Me) and silyl ketimine acetals react with aryl bromides in the presence of substoichiometric amounts of zinc fluoride, Pd(dba)2, and P(t-Bu)3 to give α-aryl esters and amides. The experimental process involved the reaction of tert-Butyl 2-(4-nitrophenyl)acetate(cas: 29704-38-9).Formula: C12H15NO4

The Article related to zinc enolate aryl bromide arylation, aryl ester preparation, amide aryl preparation, palladium arylation catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Formula: C12H15NO4

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

On August 18, 2010, Qin, Lijin; Cui, Hongmeng; Zou, Dapeng; Li, Jingya; Wu, Yangjie; Zhu, Zhiwu; Wu, Yusheng published an article.COA of Formula: C12H14F3NO2 The title of the article was Pd-catalyzed amidation of aryl(Het) halides with tert-butyl carbamate. And the article contained the following:

Pd-catalyzed cross-coupling reaction of tert-Bu carbamate with various aryl(Het) halides with Cs2CO3 as base in 1,4-dioxane as solvent was investigated, which resulted in the formation of the desired compounds in moderate to excellent yields. 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 aryl carbamate preparation, butyl carbamate aryl halide amidation palladium, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.COA of Formula: C12H14F3NO2

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

On June 15, 2012, Ma, Fangfang; Xie, Xiaomin; Zhang, Lei; Peng, Zhiyong; Ding, Lina; Fu, Lei; Zhang, Zhaoguo published an article.Category: esters-buliding-blocks The title of the article was Palladium-catalyzed amidation of aryl halides using 2-dialkylphosphino-2′-alkoxyl-1,1′-binaphthyl as ligands. And the article contained the following:

Palladium-catalyzed intermol. C-N bond-forming reactions between aryl halides and amides are described using 2-dialkylphosphino-2′-alkoxyl-1,1′-binaphthyl, which is both bulky and electron-rich, as the ligand. A variety of amides, including aliphatic and aromatic primary amides, lactams, and carbamates, e. g., I, II and III were viable substrates for the amidation, which exhibited good functional group compatibility. By tuning the substituents at the 2,2′-position of 1,1′-binaphthyl of the ligand, the palladium-catalyzed amidation of bulky aryl halides was realized and this coupling reaction was used to synthesize 2-amino-2′-methoxy-1,1′-binaphthyl in high yield. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Category: esters-buliding-blocks

The Article related to amide preparation, aryl halide amide amidation pd binaphthyl ligand, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Category: esters-buliding-blocks

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