专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
专利号:WO-2020253243-A1 优先权日:2019-06-20 标题:Process method for catalyzed synthesis of lactide with alkali metal compound 发明人:JIANG WEI; ZHANG YANKAI; SUN PING; LI AIMIN; CHEN JINLONG; ZHANG QUANXING 权利人:NANJING UNIVERSITY OF TECHNOLOGY; NANJING QUANKAI RES INSTITUTE OF BIOMATERIALS CO LTD 摘要:The present invention provides a process method for catalyzed synthesis of lactide with an alkali metal compound, comprising: mixing an alkali metal compound with a lactic acid oligomer, and carrying out a cracking reaction to obtain lactide by means of vacuum distillation, wherein the alkali metal compound used is one or a plurality of an alkali metal carbonate, an alkali metal bicarbonate, and an alkali metal hydroxide. Compared with the prior art, the advantages of the present invention is that the alkali metal compound reacts and dissolves quickly after being added to the system avoiding the problem of pipeline blocking due to a catalyst not dissolving, the alkali metal compound used is cheap and readily available, the amount of the catalyst used is small, the yield of the reaction product lactide is greater than 80%, and the reaction is rapid and easy to industrialize.
专利号:WO-2020253244-A1 优先权日:2019-06-20 标 题 :Process for catalytic synthesis of lactide 发明人:JIANG WEI; ZHANG YANKAI; SUN PING; LI AIMIN; ZHANG QUANXING 权利人:NANJING UNIVERSITY OF TECHNOLOGY; NANJING QUANKAI RES INSTITUTE OF BIOMATERIALS CO LTD 摘要:The present invention provides a process for the catalytic synthesis of lactide, comprising: mixing a lactic acid oligomer with a composite catalyst; and synthesizing lactide under a heating condition, and collecting the product using a vacuum distillation mode. The used composite catalyst is composed of a zinc or tin compound and an alkali metal compound. Compared with the prior art, the advantages of the present invention are that: the used composite catalyst features a high production rate with a small use amount, a low reaction temperature (150-220°C), and a short reaction time (2-5 h), has a single pass yield that may reach 95% or more, reduces energy consumption compared with the prior art, and facilitates industrial implementations.
专利号:US-7301006-B2 优先权日:2002-07-16 标 题 :Methods and materials for the synthesis of modified peptides 发明人:YOUNG TRAVIS G; KIESSLING LAURA L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.
专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-6013829-A 优先权日:1996-02-05 标 题 :Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl -3- phenyl propanoic acid, application to the synthesis of N-(mercaptoacyl) amino acid derivatives 发明人:DANVY DENIS; MONTEIL THIERRY; DUHAMEL PIERRE; DUHAMEL LUCETTE; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES; NOEL-LEFEBVRE NADINE; GROS CLAUDE; PLAQUEVENT JEAN-CHRISTOPHE 权利人:BIOPROJET SOC CIV 摘要:PCT No. PCT/FR97/00218 Sec. 371 Date Nov. 26, 1997 Sec. 102(e) Date Nov. 26, 1997 PCT Filed Feb. 4, 1997 PCT Pub. No. WO97/29086 PCT Pub. Date Aug. 14, 1997Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in: a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride; b) preparing the monoacetates (VII R) or (VII S) respectively; c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R); d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R); e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R1SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).