📜Methyl Carbonimidodithioic Acid Dimethyl Ester置于乙醇,氨体系中,化学反应生成 甲胍 参考文献:Schenck,Archiv Der Pharmazie,1911,Vol. 249,P. 469 标题:Schenck,Archiv Der Pharmazie,1911,Vol. 249,P. 469
专利信息
专利号:WO-9312076-A1 优先权日:1991-12-13 标题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS ROY 权利人:CORVAS INT INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-6639059-B1 优先权日:1999-03-24 标 题 :Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.
专利号:US-6734291-B2 优先权日:1999-03-24 标题:Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs
专利号:US-7173021-B2 优先权日:2004-09-02 标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers 发明人:WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA 权利人:TIANJIN NORTH PHARM SCI TECH C 摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
参考标题:Cui-Catalyzed Amination Of Arylhalides With Guanidines Or Amidines: A Facile Synthesis Of 1-H-2-Substituted Benzimidazoles 作者:Xiaohu Deng,Heather Mcallister,Neelakandha S. Mani |发布日期:2009.8.7 摘要:Cui/l5 (N,N′-Dimethylethylenediamine) Proves To Be An Efficient Catalyst System For The Amination Of Arylhalides With Guanidines. The Same Catalyst System Is Then Successfully Applied To The One-Step Synthesis Of 1-H-2-Amino-Benzimidazoles Through Tandem Aminations Of 1,2-Dihaloarenes In Modest Yields. This Methodology Is Also Applicable For The Preparation Of 1-H Or 1-Substutituted 2-Aryl- Or 2-Alkyl-Benzimidazoles
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 193. 摘要:Zentralblatt fuer Physiologie., 25(441), 1911 参考文献:10.1159/000189134 摘要:Nakamura K, Ienaga K, Nakano K, Nakai M, Nakamura Y, Hasegawa G, Sawada M, Kondo M, Mori H, Kanatsuna T. Diabetic renal failure and serum accumulation of the creatinine oxidative metabolites creatol and methylguanidine. Nephron. 1996;73(4):520–5. doi: 10.1159/000189134. 参考文献:10.1080/15216549600201622 摘要:Mori A, Kohno M, Masumizu T, Noda Y, Packer L. Guanidino compounds generate reactive oxygen species. Biochem Mol Biol Int. 1996 Sep;40(1):135–43. doi: 10.1080/15216549600201622. 参考文献:10.1021/jo016182c 摘要:Jackson MD, Gould SJ, Zabriskie TM. Studies on the formation and incorporation of streptolidine in the biosynthesis of the peptidyl nucleoside antibiotic streptothricin F. J Org Chem. 2002 May 03;67(9):2934–41. doi: 10.1021/jo016182c.