Tag: 200-300

Rosowsky, Andre; Forsch, Ronald; Uren, Jack; Wick, Michael published an article in 1981, the title of the article was Methotrexate analogs. 14. Synthesis of new γ-substituted derivatives as dihydrofolate reductase inhibitors and potential anticancer agents.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate And the article contains the following content:

The γ-tert-butyll ester (I) [79640-76-9], γ-hydrazide (II) [79640-75-8], γ-butylamide (III) [79640-74-7], and γ-benzylamide (IV) [71074-45-8] derivatives of methotrexate (MTX) were synthesized from 4-amino-4-deoxy-N10-methylpteroic acid  [19741-14-1] and the appropriate blocked L-glutamic acid precursors with the aid of the peptide bond forming reagent di-Et phosphorocyanidate. The affinity of these side chain modified products for dihydrofolate reductase  [9002-03-3] from Lactobacillus casei and L1210 mouse leukemic cells was determined spectrophotometrically or by competitive radioligand binding assay, and their cytotoxicity was evaluated against L1210 leukemic cells in culture. The results provide continuing support for the view that the γ-terminal region of the MTX side chain is an attractive site for mol. modification of this anticancer agent. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to methotrexate analog preparation anticancer, dihydrofolate reductase inhibitor methotrexate analog, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

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

Srinivas, Avula; Karthik, Pulluri; Sunitha, Malladi; Reddy, Koduri Vasumathi published an article in 2019, the title of the article was Microwave-assisted synthesis and anticancer activity of triazolyl thiazolidine derivatives of pyrene.Synthetic Route of 2873-29-2 And the article contains the following content:

In a one pot procedure a series of (R)-2-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro- 2H-pyran-2-yl)-3-phenylthiazolidin-4-ones 9a-g and 2-((2R)-2-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol- 4-yl)methoxy)-3,6-dihydro-2H-pyran-2-yl)-4-oxo-3-phenylthiazolidin-5-yl)acetic acids 10a-g was prepared by condensation of (2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro-2H-pyran-2-carbaldehyde with mercapto acids and primary amines in the presence of ZnCl2 under both microwave irradiation and conventional heating conditions. Characterization of new compounds has been done by means of IR, NMR, MS and elemental anal. The cytotoxicity was assessed against a panel of four different human tumor cell lines: A549 derived from human alveolar adenocarcinoma epithelial cells (ATCC NumberCCL-185), Hela derived from human cervical cancer cells (ATCC NumberCCL-2), MDA-MB-231 derived from human breast adenocarcinoma cells (ATCC NumberHTB22) and HEK 293 (normal human embryonic kidney cell line) using the MTT assays. Among the tested compounds 9e and 10e showed the most potent activity against MCF-7 breast cancer cell line with IC50 values of 1.91 and 1.95μM, whereas 9b, 10b, 9g and 10g showed promising activity against MDA-MB-231 and Hela cell lines with IC50 values of 5.84, 5.74, 7.89 and 7.65μM, resp. 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).Synthetic Route of 2873-29-2

The Article related to breast adenocarcinoma cervical cancer microwave anticancer pyrene triazolyl thiazolidine, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 2873-29-2

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

On January 29, 2004, Bergnes, Gustave; Smith, Whitney W.; Yao, Bing; Morgans, David J., Jr.; MacDonald, Andrew published a patent.COA of Formula: C10H19NO4 The title of the patent was Preparation of of quinazolinone-like derivatives to treat cellular proliferative diseases. And the patent contained the following:

The invention relates to quinazolinone-like derivatives that are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. Preparation of 3-Benzyl-7-chloro-2-(3-benzyl-2-oxohexahydropyrimidin-4-yl)-3H-quinazolin-4-one is included. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).COA of Formula: C10H19NO4

The Article related to quinazolinone derivative preparation proliferative disease kinesin, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.COA of Formula: C10H19NO4

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

On September 4, 2012, Degrado, William F.; Bennett, Joel S.; Snyder, Seth Elliott; Choi, Sungwook published a patent.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Inhibitors of the α2β1/gpia-iia integrin. And the patent contained the following:

Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2β1/GPIa-IIa-mediated activity. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to prolyl peptide preparation inhibitor integrin, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

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

On December 14, 2006, Degrado, William F.; Bennett, Joel S.; Snyder, Seth Elliot; Choi, Sungwook published a patent.Application In Synthesis of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Preparation of prolyl dipeptides as inhibitors of the α2β1/gpIa-IIa integrin. And the patent contained the following:

The invention discloses novel compounds I [X is alkylidene; R1 is aralkylamino, aryl- or alkylsulfonylamino, carbalkoxymethyl, aralkoxycarbonylamino, NHSO2R2, where R2 is aryl, alkyl, aralkyl, aralkoxy, aralkylamino, arylamino, or alkylamino; R3 is halo, nitro, aryl, amino, alkyl, alkoxy, alkylsulfonyl, etc.; R4 is amino, hydroxy, aralkoxy, arylamino, aroylamino; R5 is H or alkyl; R6 is H or :O; A is SO2, PO2, CO2, CO; D is optional and may be one or more CH2 groups; E is aryl or heteroaryl; n, q are 0-2; m is 0 or 1; one of the three dashed-line portions may represent a double bond] or a stereoisomer, prodrug, pharmaceutically-acceptable salt, or N-oxide, which inhibit the integrin α2β1/GPIa-IIa receptor and are useful for the treatment of α2β1-affected disease states. Thus, prolyl peptide II was prepared and showed IC50 = 15 nM for inhibition of platelet adhesion to type I collagen. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Application In Synthesis of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to prolyl peptide preparation inhibitor integrin, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Application In Synthesis of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

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

On January 17, 1984, Meienhofer, Johannes A. published a patent.Application of 53838-27-0 The title of the patent was Immunopotentiating peptides. And the patent contained the following:

Peptides H-X-Glu-Asn-OH [X = null, Ala (I), Glu-Glu-Ala (II), Val-Glu-Glu-Ala, Val-Val-Glu-Glu-Ala] and their salts were prepared by known procedures. These di- to heptapeptides represent fragments of thymosin α1. Thus, I and II were prepared from their benzyl-protected derivatives by hydrogenolysis. I and II showed activity comparable to that of thymosin α1 in converting precursor T cells into steroid sensitive T1 cells or steroid resistant T2 cells. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Application of 53838-27-0

The Article related to immunopotentiation thymosin peptide fragment, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Application of 53838-27-0

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

Fagge, Ibrahim I.; Ahmad, W. Hamdah W.; Zain, Sharifuddin Md; Khan, M. Niyaz published an article in 2018, the title of the article was Kinetics and mechanism of counterionic salt-catalysed piperidinolysis of anionic phenyl salicylate in the presence of cationic-nonionic mixed micelles.Application In Synthesis of Phenyl Salicylate And the article contains the following content:

The quant. correlation of counterion-affinity to aqueous hexadecyltrimethylammonium bromide (HDAB, cationic micelles/nanoparticles) and the counterion-induced HDAB micellar growth, in the presence of different amounts of poly(ethylene glycol hexadecyl ether) (C16E20, nonionic surfactant), was achieved by the use of a semi-empirical kinetic (SEK) method. The values of the ratio of cationic HDAB, as well as mixed HDAB-C16E20, micellar binding constants of X and Br, KX/KBr (= KBrX or RBrX) for X = 4-ClC6H4CO2-, were obtained by the SEK method. The concentration range (0.006-0.015 M) of pure HDAB was found to have no influence on the values of KBrX or RBrX. These observations were also recorded upon addition of a nonionic surfactant, C16E20, in an aqueous solution of HDAB. The mean value of KBrX or RBrX obtained in the presence of pure HDAB (KBrX or RBrX = 50.3) is 2.3 times larger than that in the presence of mixed HDAB-C16E20 (mKBrX or mRBrX = 21.7). From rheometric measurements of aqueous HAD+/4-ClC6H4CO2- with 0.015 M HDAB, single sym. maxima (at both 25 and 35 °C) were obtained at [4-ClC6H4CO2Na] = 0.03 M. This is evidence for the existence of wormlike micelles/nanoparticles. However, the absence of a maximum in rheometric data for aqueous HAD+/C16E20/4-ClC6H4CO2- with 0.015 M HDAB and 0.006 M C16E20 at various [4-ClC6H4CO2Na] revealed the existence of spherical micelles. The experimental process involved the reaction of Phenyl Salicylate(cas: 118-55-8).Application In Synthesis of Phenyl Salicylate

The Article related to phenyl salicylate piperidinolysis kinetics, Physical Organic Chemistry: Other Reactions, Processes, and Spectra and other aspects.Application In Synthesis of Phenyl Salicylate

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

On August 31, 1985, Felix, Arthur M.; Heimer, Edgar P.; Wang, Ching Tso; Lambros, Theodore J.; Swistok, Joseph; Roszkowski, Martin; Ahmad, Mustaq; Confalone, Dianne; Scott, John W. published an article.Product Details of 53838-27-0 The title of the article was Synthesis of thymosin α1 by fragment condensation using tert-butyl side chain protection. And the article contained the following:

Thymosin α1 (I) was prepared by classical methods using 7 tert-Bu side chain protected fragments. Optimum conditions were found for the final DCC/HOBt coupling of the two key intermediates; decapeptide and octadecapeptide. I was purified by two stages of preparative HPLC (partial purification with C8 and final purification with C18 reverse phase silica gel) to give a 30% overall yield for the final four stages of synthesis (including catalytic hydrogenation of octadecapeptide, coupling, deprotection and purification). The product was homogeneous according to thin-layer and paper high voltage electrophoresis, isoelec. focusing anal., thin-layer chromatog. and high-performance liquid chromatog. Amino acid anal., optical rotation, 1H NMR spectroscopy, FAB mass spectroscopy and peptide mapping after tryptic digestion confirmed the structure of thymosin α1. Three minor stereoisomer contaminants were isolated by HPLC and characterized as [D-Lys14]-thymosin α1, [D-Lys17]-thymosin α1 and [D-Ala3]-thymosin α1 resulting from racemization at Lys14, Lys17 and Ala3 during the coupling of the fragments. A final contaminant, isolated by HPLC, was characterized as Nα-isobutyloxycarbonyl-thymosin α1 (15-28), which results from “wrong way opening” of an activated mixed anhydride. 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 thymosin synthesis fragment condensation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Product Details of 53838-27-0

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

On August 26, 2016, Malolanarasimham, Krishnan; Murugan, Ravichandran Narayanasamy; Kedari, Chaitanya Kumar; Tulam, Vijaya Kumar published a patent.Safety of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Acylation process for the preparation of liraglutide. And the patent contained the following:

The invention is related to a process for the preparation of an N-substituted peptide or protein comprising: (a) reacting a peptide or protein with a copper agent to form a copper complex of peptide or protein; (b) converting the copper complex of the peptide or protein obtained in step (a) to the desired N-substituted peptide or protein in an organic solvent or in water or mixtures thereof; and (c) optionally, hydrolyzing the N-substituted peptide or protein obtained in step (b) to obtain the desired N-substituted peptide or protein, wherein the N-substituted peptide or protein is the GLP agonist H-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-N6 -[N-(1-oxohexadecyl)-γ-Glu]-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH (liraglutide). The invention provides an alternate acylation process for preparation of liraglutide high yielding, scalable, cost effective, environment friendly and com. viable by avoiding repeated cumbersome and lengthy purification steps. Specifically, the invention is related to process for the preparation of liraglutide comprising: (i) reacting a liraglutide precursor with a copper agent, e.g., CuSO4•5H2O to form a copper complex of liraglutide precursor, (ii) converting the copper complex of liraglutide precursor obtained in step (i) to N-substituted liraglutide precursor by reacting with an N-acylating agent such as 1-Me palmityl glutamic acid or its reactive derivatives (preparation given); and (iii) hydrolyzing the N-substituted liraglutide precursor obtained in step (ii) to obtain liraglutide. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Safety of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to acylation liraglutide preparation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Safety of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

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

On November 30, 1983, Naithani, Vinod K.; Schwertner, Eberhard published an article.Related Products of 53838-27-0 The title of the article was Human proinsulin VI. Synthesis of protected segment 46-70 of prohormone. And the article contained the following:

Title protected peptide Ph3C-Gly-Gly-Pro-Gly-Ala-Gly-Ser(CMe3)-Leu-Gln-Pro-Leu-Ala-Leu-Glu(OCMe3)-Gly-Ser(CMe3)-Leu-Gln-Lys(CO2CMe3)-Arg-Gly-Ile-Val-Glu(OCMe3)-Gln-OH was prepared by a series of fragment condensations in solution The final step involved 2 possible mixed anhydride condensations: the coupling of protected fragment 46-64 with protected fragment 65-70 or the coupling of protected fragment 46-59 with protected fragment 60-70. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Related Products of 53838-27-0

The Article related to proinsulin pentacosapeptide, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Related Products of 53838-27-0

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