专利号:US-9242925-B2 优先权日:2011-08-29 标题:Versatile and stereospecific synthesis of γ,δ-unsaturated amino acids by Wittig reaction 发明人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE 权利人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE; CENTRE NAT RECH SCIENT; UNIV BOURGOGNE 摘要:The γ,δ-unsaturated α-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). n n n n n n n n n n n n Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.
专利号:US-2015148524-A1 优先权日:2012-07-06 标题:Amino acid analogues and methods for their synthesis 发明人:WANG ZHEN; ROBINSON ANDREA; SPICCIA NICOLAS DANIEL; JACKSON WILLIAM ROY 权利人:UNIV MONASH 摘要:A method for the synthesis of an amino acid analogue or a salt, solvate, derivative, isomer or tautomer thereof comprising the steps of: (i) subjecting an amino acid containing a metathesisable group to metathesis with a compound containing a complementary metathesisable group of formula (I) or (II): (Formulae (I), (II)) wherein R 1 and R 2 are independently selected from H and substituted or unsubstituted C 1 to C 4 alkyl; each R 3 is either absent or independently selected from a heteroatom, a substituted or unsubstituted C 1 to C 20 alkyl, and a substituted or unsubstituted C 1 to C 20 alkyl group interrupted by one or more heteroatoms; and each X is independently selected from H and an effector molecule; in the presence of a reagent to catalyse the metathesis to form a dicarba bridge between the amino acid containing a metathesisable group and the compound containing a complementary metathesisable group; and (ii) reducing the dicarba bridge to form a saturated dicarba bridge, wherein the reagent used to catalyse step (i) also catalyses step (ii).
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:US-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:WO-9710221-A1 优先权日:1995-09-15 标 题:Synthesis of quinazolinone libraries 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TORREY PINES INST 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.