专利号:US-12162849-B2 优先权日:2018-12-21 标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.
专利号:US-2007293706-A1 优先权日:2004-11-01 标 题:Synthesis Of 1,5-Disubstituted-2-Hydroxy-Gibbatetraen-6-Ones 发明人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 权利人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 摘要:1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Robinson-type annulation followed by an internal alkylation reaction. This invention further describes the novel use of a fluoroethyl substituent as a latent alkylating group for an internal cyclization reaction.
专利号:US-10745354-B2 优先权日:2017-11-01 标题 :Methods for enantioselective allylic alkylation of esters, lactones, and lactams with unactivated allylic alcohols 发明人:STOLTZ BRIAN M; NGAMNITHIPORN AURAPAT; JETTE CARINA I; BACHMAN SHOSHANA; VIRGIL SCOTT C; LACKNER SEBASTIAN 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic α-quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.
专利号:WO-2007093765-A1 优先权日:2006-02-13 标题 :Process for the cyanation of aldehydes 发明人:NORTH MICHAEL; BELOKON YURI 权利人:NPIL PHARMACEUTICALS UK LTD; NORTH MICHAEL; BELOKON YURI 摘要:The present invention relates to a process for the cyanation of aldehydes, particularly to the asymmetric cyanation of aldehydes, including the synthesis of chiral cyanohydrins and derivatives thereof, such as chiral O-acyl cyanohydrins. The process of the present invention comprises: reacting the aldehyde with a cyanating agent in the presence of a chiral catalyst and less than a stoichiometric amount of an ionic cyanide source. Chiral catalysts employed in the process according to the present invention are of the formula: (1), (3a), (3b).
专利号:US-9303046-B2 优先权日:2012-08-07 标 题:Process for the preparation of heterocyclic ester derivatives 发明人:BONGARTZ JEAN-PIERRE ANDRÉ MARC; STAPPERS ALFRED ELISABETH; TELEHA CHRISTOPHER A; WEERTS KOEN JOHAN HERMAN; WILSON KENNETH J 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to a process for the preparation of heterocyclic ester derivatives of formula I n nwherein A 1 , SEM, and W 1 are as defined herein. Such compounds are useful as intermediates in the synthesis of derivatives useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.
专利号:US-6982331-B2 优先权日:2001-06-08 标 题 :Synthesis of chlorinated pyrimidines 发明人:DOYLE TIMOTHY J; BENKE ALAN H; WEHRENBERG PETER K; NADY LOUIE A; RODRIGUEZ GILBERT 权利人:SYNGENTA CROP PROT INC 摘要:The invention provides a process for synthesizing chlorinated pyrimidines. The process includes reacting imidoyl chloride compounds with phosgene (COCl 2 ). The imidoyl chloride compounds can be supplied as starting materials or can be produced by reacting organic amides with phosgene or reacting organic nitrites with hydrogen chloride. Phosgene may be replaced by equivalent reagents. The chlorinated pyrimidines, such as 4,6-dichloropyrimidine, can be used to synthesize other compounds useful in a variety of compositions, such as fungicides, pesticides, and pharmaceuticals.