专利号:US-2025188046-A1 优先权日:2023-12-08 标题:Ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent sufex connections via lithiated chemistry 发明人:KIM DONG-PYO; KANG JI-HO 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:Disclosed are ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent SuFEx connections via lithiated chemistry. In detail, a method of synthesizing an ortho-functionalized benzenesulfonyl fluoride derivative, the method comprises (a) reacting a benzenesulfonyl fluoride derivative represented by structural formula 1 with an organolithium represented by structural formula 2, thus synthesizing an intermediate represented by structural formula 3 in reaction scheme 1 and (b) reacting the intermediate with an electrophile, thus synthesizing a compound represented by structural formula 4 or a compound represented by structural formula 4′. The present disclosure enables the synthesis of several functionalized sulfonyl fluorides within a few seconds under mild temperature conditions in addition to the chemistry of Sulfonyl Fluoride Exchange (SuFEx), which is a next-generation click chemistry, so that sulfonyl fluoride, the main reactant of the SuFEx reaction, can be efficiently secured.
专利号:US-6489507-B1 优先权日:1999-06-11 标题:Process for the synthesis of 3,5-bis(trifluoromethyl)benzoic acid 发明人:CVETOVICH RAYMOND; LEAZER JOHN 权利人:MERCK & CO INC 摘要:The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)benzoic acid (CAS 725-89-3). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.
专利号:US-2023167051-A1 优先权日:2020-02-25 标 题 :A PROCESS FOR SYNTHESIS OF HIGH PURITY l-[3-(TRIFLUOROMETHYL)PHENYL]ETHANONE OXIME 发明人:GOENKA RAVI; AUDI AJAY A 权利人:LAXMI ORGANIC IND LTD 摘要:A process for preparation of 3-Trifluoromethyl acetophenone oxime of formula I includes reacting an isomeric mixture of halo benzotrifluoride with Mg metal in an organic solvent in presence of a catalyst to obtain a Grignard complex. The Grignard complex is reacted with a ketene in hydrocarbon solvent in presence of transition metal ligand-acid complex to obtain an isomeric mixture of trifluoromethyl acetophenone. Finally, the isomeric mixture of trifluoromethyl acetophenone is reacted with hydroxylamine salt to obtain compound of formula I.
专利号:US-2003153760-A1 优先权日:1999-07-01 标 题 :Process for the synthesis of (R)-1-(3,5-bis(trifluoromethyl)-phenyl)ethan-1-ol by asymmetric transfer hydrogenation
专利号:US-2023099421-A1 优先权日:2019-12-17 标题 :A new method of 18f labelling and intermediate salts 发明人:YOUNG ROWAN DRURY; MANDAL DIPENDU; GUPTA RICHA; JAISWAL AMIT KUMAR 权利人:NAT UNIV SINGAPORE 摘要:Disclosed herein is a salt of formula I: where R 1 , X, n, R, R 1 , Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET & imaging, as well as methods to make the compounds of formula I.
专利号:US-2011301143-A1 优先权日:2009-02-23 标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ•?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.