CAS: 82834-12-6; N-[(S)-1-Carbethoxy-1-Butyl]-L-Alanine

相似化合物

145682-38-8 760127-31-9 82834-11-5

上下游产品

-L-alanine benzyl esterN-1(S)-(ethoxycarbonyl)butyl-L-alanine benzyl ester ethyl 2-hydroxy-n-valerate ethyl 2-([(trifluoromethyl)sulphonyl]oxy)pentanoate sodium pyruvate(2S,3aS,7aS)-1-{2-[1-ethoxycarbonyl-(S)-butylamino]-(S)-propionyl}-°Ctahydroindole-2-carboxylic acid p-nitrobenzylic ester (2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)butyl]amino]-1-oxopropyl]°Ctahydro-1H-indole-2-carboxylic acid benzyl ester Perindopril N,N-dicyclohexylurea

2-羟基戊酸乙酯置于palladium On Activated Charcoal 吡啶,氢气,三乙胺体系中,用 乙醇,二氯甲烷 作为反应溶剂,-22.0~25.0 °C,303.98 Kpa 条件下,反应 18.75H,反应生成 N-[(S)-乙氧羰基-1-丁基]-(S)-丙氨酸
参考文献:一种新型的,构象受限的,含2,3-二氢-1,3,4-噻二唑的血管紧张素转化酶抑制剂的设计,合成和理化性质,其优选通过大鼠的胆道途径消除.
标题:一种新型的,构象受限的,含2,3-二氢-1,3,4-噻二唑的血管紧张素转化酶抑制剂的设计,合成和理化性质,其优选通过大鼠的胆道途径消除.
摘要:设计并合成了两个新系列的含二氢噻二唑环的血管紧张素转化酶抑制剂.该化合物是高效的酶抑制剂,并且由于构象限制,对于不希望的环化反应而言是化学稳定的.该系列中最有趣的化合物5A(fpl 63547)是高效的"氨基羧基"抑制剂5B(fpl 63674)的单乙酯前药.口服给药后,可在动物模型中长期产生降压作用.与其他ace抑制剂不同,大鼠体内的胆汁清除几乎消除了5B.根据5A和5B的独特理化特性,合理化了其药理特性.用5B观测到的对胆道清除的明显偏爱与其亲脂性和在生理ph下的高净离子化程度相一致,这是由于c端羧酸功能的pka值非常低所致.fpl 63547目前正在人体中进行临床研究.
DOI:10.1021/jm00105A066

专利信息

专利号:US-7323575-B2
优先权日:2003-04-09
标题:Process for the synthesis of (2S)-indoline-2-carboxylic acid
发明人：SOUVIE JEAN-CLAUDE; LECOUVE JEAN-PIERRE
权利人:SERVIER LAB
摘要:Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): n nApplication in the synthesis of perindopril and its pharmaceutically acceptable salts.

专利号:US-6774259-B2
优先权日:2000-04-11
标 题 :Method for synthesis of n-[(s)]-1-carboxybutyl-(s)-alanine esters and use in synthesis of perindopril
发明人：SOUVIE JEAN-CLAUDE; RENAUD ALAIN
权利人:SERVIER LAB
摘要:A stereoselective process for the industrial synthesis of compounds of formula (I):wherein R represents linear or branched (C1-C6)alkyl, andapplication in the synthesis of perindopril and pharmaceutically acceptable salts thereof.

专利号:US-6818788-B2
优先权日:2000-03-31
标 题:Method for synthesis of n-[(s)-1-carboxybutyl]-(s)-alanine esters and use in synthesis of perindopril
发明人：SOUVIE JEAN-CLAUDE
权利人:SERVIER LAB
摘要:Stereoselective process for the industrial synthesis of compounds of formula (I):wherein R represents linear or branched (C1-C6)alkyl.Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.

专利号:US-4902817-A
优先权日:1987-09-17
标 题 :Process for the synthesis of alpha n alkylated amino acids and esters thereof, application to the synthesis of carboxyalkyl dipeptides
发明人：VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES
权利人:ADIR
摘要:Stereoselective process for the industrial synthesis of compounds of formula (I): ##STR1## where R 1 is linear or branched lower alkyl with 1 to 6 carbon atoms, n R 2 is a linear or branched lower alkyl with 1 to 4 carbon atoms, n employing inexpensive starting materials and obtaining optimum yields. n Application to the synthesis of carboxyalkyl dipeptides.

专利号:EP-0309324-B1
优先权日:1987-09-17
标 题:Process for the preparation of n-alkylated amino acids and their esters, use in the synthesis of carboxyalkyl dipeptides
摘要:Process for industrial synthesis of the derivative of formula (I): and their addition salts with an inorganic or organic acid or base, in which: R1 is linear or branched lower alkyl (of 1 to 6 carbon atoms), R2 is hydrogen or a linear or branched lower alkyl group (of 1 to 4 carbon atoms). Application to the industrial synthesis of carboxyalkyl dipeptides.

专利号:US-7060842-B2
优先权日:2001-07-24
标题 :Method for synthesis of (2S, 3aS, 7aS)-1-{(S)-alanyl}-octahydro-1H -indole-2-carboxylic acid derivatives and use for synthesis of perindopril
发明人：MEZEI TIBOR; PORCS-MAKKAY MARTA; SIMIG GYULA
权利人:SERVIER LAB
摘要:Process for the industrial synthesis of the compounds of formula (I): n nwherein R 1 represents a hydrogen atom or an alkyl or benzyl group, and R 2 represents a group that protects the amino function.