CAS: 74863-84-6; (2R,4R)-1-((2S)-5-Guanidino-2-(3-Methyl-1,2,3,4-Tetrahydroquinoline-8-Sulfonamido)Pentanoyl)-4-Methylpiperidine-2-Carboxylic Acid

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CAS号74874-10-5 (2R,4R)-1-[(2S)... | CAS号367952-84-9 benzyl (2R,4R)-... | CAS号626-58-4 4-甲基哌啶 | CAS号123387-50-8 4-甲基哌啶-1-甲酸叔丁酯 | CAS号74863-82-4 3-甲基喹啉-8-磺酰氯 | CAS号367952-82-7 (2R,4R)-1-[(2S)...

1-Boc-4-甲基哌啶置于palladium On Activated Charcoal 盐酸,四甲基乙二胺,氢气,仲丁基锂,三乙胺体系中,用 乙醚,乙醇,二氯甲烷,溶剂黄146,乙酸乙酯 作为反应溶剂,-90.0~20.0 °C,101.33 Kpa 条件下,反应 20.0H,反应生成 阿加曲班
参考文献:A Short Synthesis Of Argatroban
标题:A Short Synthesis Of Argatroban
摘要:Argatroban Was Synthesized In Seven Steps From 4-Methylpiperidine. The Condensation Of (+/-)-Trans-Benzyl 4-Methyl-Pipecolic Acid Ester With N-Alpha-Boc-N-Omega-Nitro-L-Arginine Led To Two Diastereomers That Were Separated. One Of Them Is The Precursor Of Argatroban. (C) 2001 Elsevier Science Ltd. All Rights Reserved.
DOI:10.1016/s0960-894X(01)00351-1

专利信息

专利号:US-9994526-B2
优先权日:2011-04-04
标 题 :Process intermediates and methods for the preparation of process intermediates for the synthesis of argatroban monohydrate
发明人：STIVANELLO MARIANO; HUBER FLORIAN ANTON MARTIN; RICCI ANTONIO
权利人:LUNDBECK PHARMACEUTICALS ITALY S P A
摘要:Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.

专利号:US-9630923-B2
优先权日:2013-07-09
标题:Biocatalyzed synthesis of the optically pure (R) and (S) 3-methyl-1,2,3,4-tetrahydroquinoline and their use as chiral synthons for the preparation of the antithrombic (21R)- and (21S)-argatroban
发明人：GRISENTI PARIDE
权利人:EUTICALS SPA; EUTICALS SPA
摘要:The present invention relates to the biocatalyzed synthesis of enantiomerically pure (3R) and (3S)-methyl-1,2,3,4-tetrahydroquinoline. Said enantiomerically pure compounds are useful as chiral synthons in organic synthesis and, in particular, for the preparation of diastereomerically pure (21R) and (21S)-agratroban and its analogs. New compounds used as intermediates in the process of the invention are also disclosed.

专利号:US-8378106-B2
优先权日:2008-04-07
标题:Method for preparing argatroban monohydrate and a process for its synthesis
发明人：ZANON JACOPO; LIBRALON GIOVANNA; NICOLE ANDREA
权利人:LUNDBECK PHARMACEUTICALS ITALY S P A; ZANON JACOPO; LIBRALON GIOVANNA; NICOLE ANDREA
摘要:A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[N G -nitro-N 2 -(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2-piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico-chemical characteristics. n The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.

专利号:US-2014088310-A1
优先权日:2011-04-04
标 题 :Process intermediates and methods for the preparation of process intermediates for the synthesis of argatroban monohydrate

专利号:CA-2831987-C
优先权日:2011-04-04
标 题 :Method for the preparation of process intermediates for the synthesis of argatroban monohydrate

专利号:CA-2960667-A1
优先权日:2011-04-04
标题:Method for the preparation of process intermediates for the synthesis of argatroban monohydrate