专利号:US-4599198-A 优先权日:1985-08-02 标题 :Intermediates in polypeptide synthesis 发明人:HOOVER DENNIS J 权利人:PFIZER 摘要:Bis(t-butoxycarbonyl) derivatives of phenylalanylhistidine as intermediates in the synthesis of rennin inhibiting polypeptides.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:WO-2006100479-A1 优先权日:2005-03-22 标题:Methods for the synthesis of heteroaromatic compounds 发明人:KNIGHT DAVID W 权利人:UNIV CARDIFF; KNIGHT DAVID W 摘要:Methods of making heteroaromatic compounds comprising a 5- membered ring, and dihydro forms thereof, by a metal catalysed 5-endo-cyclisation of alkynes (acetylenes) are disclosed. The methods involve the use of a catalyst comprising a silver salt, more preferably a silver (I) salt, which is employed as a heterogeneous catalyst for the cyclisation reaction. The methods can produce different types of heteroaromatic compounds and are capable of producing highly substituted products, i.e. products in which the 5-membered ring is disubstituted, trisubstituted or, with further simple reactions, tetrasubstituted. The methods described herein generally the advantages that they use conditions and reagents that are benign, cheap and flexible and amenable to scale up, and in which the only by-product is water.
专利号:US-7951834-B2 优先权日:2005-05-27 标题 :Angiotensin I-converting enzyme (ACE) inhibitors 发明人:STURROCK EDWARD; NCHINDA ALOYSIUS; CHIBALE KELLY 权利人:UNIV CAPE TOWN 摘要:This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACEâ€?, compound 5 a ) and analogues thereof. The synthesis process proceeds via an α,β-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.
专利号:US-2003158436-A1 优先权日:1999-03-10 标题:Synthesis of alpha--amino-alpha, alpha'- dihaloketones and process for the preparation of beta--amino acid derivatives by the use of the same
专利号:US-6573399-B1 优先权日:1999-03-10 标题:Synthesis of α-amino-α′, α′-dihaloketones and process for the preparation of β-amino acid derivatives by the use of the same 发明人:NISHIYAMA AKIRA; INOUE KENJI 权利人:KANEKA CORP 摘要:The present invention provides a commercially profitable process for producing a β-amino acid ester derivative n which comprises reacting an α-amino acid ester derivative with a base and a dihalomethane, n reacting the same with a lithium amide and an alkyllithium in succession, n and treating the reaction product with an acid in an alcohol.