L-叔亮氨酸甲酯盐酸盐置于盐酸,Sodium Hydroxide,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇 作为反应溶剂,化学反应生成 (2S)-2-环己基-N-(2-吡嗪基羰基)甘氨酰-3-甲基-L-缬氨酸 参考文献:P4 And P1' Optimization Of Bicycloproline P2 Bearing Tetrapeptidyl α-Ketoamides As Hcv Protease Inhibitors 标题:P4 And P1' Optimization Of Bicycloproline P2 Bearing Tetrapeptidyl α-Ketoamides As Hcv Protease Inhibitors 摘要:With The Aim Of Improving Hcv Protease Inhibitors Reported In Our Previous Manuscripts,We Synthesized And Evaluated A Series Of La-Based Tetrapeptidyl Alpha-Ketoamides With Additional P4 Modification. The Promising Analog Discovered Through This Sar,5A,Was Further Derivatized At P1' Or P1 Position. As A Result Of These Efforts,We Found That Replacement Of The P4 Valine As Seen In 1A With Cyclohexylglycine (Chg) Resulted In The Discovery Of 5A,5C,And 5E Endowed With Improved Cellular Activity In Comparison To 1A. (C) 2004 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2004.07.007
专利号:US-8686145-B2 优先权日:2010-02-25 标 题 :Process for the preparation of α-acyloxy β-formamido amides 发明人:RUIJTER EELCO; ORRU ROMANO; ZNABET ANASS; POLAK MARLOES; TURNER NICHOLAS 权利人:RUIJTER EELCO; ORRU ROMANO; ZNABET ANASS; POLAK MARLOES; TURNER NICHOLAS; VERENIGING VOOR CHRISTELIJK HOGER ONDERWIJS WETENSCHAPPELIJK ONDERZOEK EN PATIENTENZORG C O TECHNOLO 摘要:The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R 2 COOH and a compound of the general Formula IV R 3 NC under such conditions that compound I is formed, wherein R 1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R 2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R 3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
专利号:US-2015038677-A1 优先权日:2012-03-16 标 题:Process for the synthesis of telaprevir, or pharmaceutically acceptable salts or solvates as well as intermediate products thereof 发明人:FELZMANN WOLFGANG; BRUNNER STEFANIE; WILHELM THORSTEN 权利人:SANDOZ AG 摘要:The invention relates to a process for the preparation of telaprevir, or a pharmaceutically acceptable salt or solvate thereof, wherein the process requires a smaller number of process steps and/or does not require the use of toxic and instable compounds compared to the known processes. Another embodiment refers to telaprevir, or a pharmaceutically acceptable salt or solvate thereof as well as to intermediate products for preparation of the same, wherein the afore-mentioned products are obtained by the process described herein.
专利号:WO-2013131978-A1 优先权日:2012-03-07 标 题:Process for the preparation of intermediates useful in the preparation of a viral protease inhibitor 发明人:MANTEGAZZA SIMONE; ATTOLINO EMANUELE; ALLEGRINI PIETRO 权利人:DIPHARMA FRANCIS SRL 摘要:Process for the preparation of intermediates useful in the synthesis of the viral protease inhibitor Telaprevir. The claimed process involves reacting formula (IV) with a formula (III) compound using DMMTM as coupling reagent to get a formula (II) compound.
专利号:WO-2013135870-A1 优先权日:2012-03-16 标 题:Process for the synthesis of telaprevir, or pharmaceutically acceptable salts or solvates as well as intermediate products thereof