专利号:US-7317129-B2 优先权日:2002-06-07 标 题:Chemical synthesis of reagents for peptide coupling 发明人:RAINES RONALD T; KIESSLING LAURA L; NILSSON BRADLEY L; HE YI; SOELLNER MATTHEW B; HINKLIN RONALD J 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides improved methods for synthesis of phosphinothiol reagents, as well as novel protected reagents, for use in formation of amide bonds, and particularly, for peptide ligation. The invention provides phosphine-borane complexes useful as reagents in the formation of amide bonds, particularly for the formation of an amide bond between any two of an amino acid, a peptide, or a protein.
专利号:US-10669292-B2 优先权日:2014-05-05 标 题 :Synthesis of boronate salts and uses thereof 发明人:HECKER SCOTT; BOYER SERGE 权利人:REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.
专利号:US-4713479-A 优先权日:1986-11-28 标题 :Synthesis of high-purity dialkyl 2-vinylcyclopropane-1,1-dicarboxylate 发明人:CLARK JR CLARENCE E; FAYTER JR RICHARD G 权利人:NAT DISTILLERS CHEM CORP 摘要:This invention relates to a two-step synthesis of high purity dialkyl 2-vinyl-cyclopropane-1,1-dicarboxylate in which a mixture of trans- and cis-1,4-dihalobutene-2 is first isomerized to essentially trans-1,4-dihalobutene-2 followed immediately by cyclocondensing the resultant trans-1,4-dihalobutene-2 with a malonic ester in the presence of an alcoholic solution of a metallic alkoxide.
专利号:US-7619116-B2 优先权日:2003-12-17 标 题:Intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation 发明人:DAMBRIN VALERY; LENOIR JEAN-YVES; SCHNEIDER JEAN-MARIE; GUILLAMOT GERARD; FOLLET MICHEL; BECKER ABRAM 权利人:PRODUCTS CHIMIQUES AUXILIAIRES 摘要:A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.
专利号:US-2010204449-A1 优先权日:2007-09-04 标 题 :Methods and intermediates for chemical synthesis of polypeptides and proteins 发明人:DONG ZHENG XIN; KIM SUN H 权利人:DONG ZHENG XIN; KIM SUN H 摘要:The present invention relates to methods and intermediates for chemical synthesis of polypeptides and proteins, and more particularly to methods and intermediates for chemically ligating a peptide fragment containing N-terminal β-methyl-cysteine (SEQ ID NO: 1) with another peptide fragment having C-terminal thioester to generate a β-amino-thioester intermediate that spontaneously rearranges to form an amide bond. The invention also relates to methods of synthesizing β-methyl-cysteine (SEQ ID NO: 1) and its protected forms. Furthermore, the invention relates to converting a β-methyl-thiazolidine residue to a β-methyl-cysteine (SEQ ID NO: 1) residue of polypeptides and proteins.
专利号:US-5268271-A 优先权日:1989-12-12 标题 :Method for the synthesis of semi-synthetic antibiotics in thermodynamically controlled water-cosolvent organic miscible apolar systems by using penicillin G acylase 发明人:GUISAN SEIJAS JOSE M; FERNANDEZ LAFUENTE ROBERTO; ALVARO CAMPOS GREGORIO; BLANCO MARTIN ROSA M; MOLINA ROSELL CRISTINA 权利人:CONSEJO SUPERIOR INVESTIGACION 摘要:Synthesis of semi-synthetic monobactamic or β-Lactamic antibiotics by using derivatives stabilized by various methods of penicillin G acylase from various microbial sources according to a thermodynamically controlled strategy in monophase water/cosolvent organic apolar systems, wherein the concentration of the cosolvent varies between 30% and 90%, the temperature between -10° C. and 50° C., the pH between 4.5 and 8.5, with concentrations of the antibiotic nucleus between 0.5 an 875 mM and acyl donor between 0.2 mM and 1M, with a relationship antibiotic ring/activated or free acyl donor, using a buffer between 0 and 1M. Application to the pharmaceutical industry.