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专利信息

专利号:US-10787458-B2
优先权日:2014-09-25
标 题:Chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-A]pyrazines
发明人：HOVEYDA HAMID; DUTHEUIL GUILLAUME
权利人:OGEDA SA
摘要:Disclosed is a novel chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines of Formula (I): n nor a solvate thereof. The novel chiral synthesis avoids the use of protection/deprotection steps.

专利号:US-12351558-B2
优先权日:2020-04-17
标题 :Process for the synthesis of lofexidine
发明人：NG CHOI I-TENG MONTSERRAT
权利人:MEDICHEM SA
摘要:The present invention relates to an improved process for the synthesis of lofexidine, or a pharmaceutically acceptable salt thereof, using an aluminium alkoxide as Lewis acid.

专利号:US-2024059701-A1
优先权日:2021-04-22
标 题 :Methods for Synthesis of an Advantageous N-Heterocyclic Carbene Catalyst
发明人：CAHANA AVIAD; FARONE WILLIAM A
权利人:XF TECH INC
摘要:The present invention concerns the synthesis of the salts of a Triazolium N-Heterocyclic Carbene (NHC) catalyst in various salt forms prepared from 2-methylaniline, 2-methylphenylhydrazine hydrochloride or 2-methylphenylhydrazine. The molecules so prepared are useful in catalysis of carbene reactions and are advantageous due to their lack of chlorinated or fluorinated intermediates and lack of chlorine or fluorine in the final structure.

专利号:US-5191110-A
优先权日:1987-05-21
标题 :Process for the synthesis of vitamin A and certain ones of derivatives
发明人：SOLLADIE GUY; FORESTIER SERGE; LANG GERARD
权利人:OREAL
摘要:According to this process, one effects a stereospecific reduction of the two hydroxyl groups of an ether-diol by a mixture (titanium trichloride, lithium aluminum hydride) at a temperature between 5° C. and about 40° C. and that optionally, one converts the resulting ether into vitamin A, retinol or retinoic acid. n Application to the synthesis of all-trans compounds selected from the group consisting of vitamin A and its ethers, retinol and retinoic acid, and their 13-cis isomers.

专利号:US-8580975-B2
优先权日:2008-01-11
标 题:Synthesis of macrocyclic cancer chemotherapy agents and methods of use
发明人：GHOSH ARUN K; XU XIAOMING
权利人:GHOSH ARUN K; XU XIAOMING; PURDUE RESEARCH FOUNDATION
摘要:Herein are described a process for forming a quaternary carbon useful in the preparation of macrolactones, an enantioselective synthesis of (+)-peloruside A, and methods for treating a patient in need of relief from cancer or a cancer-related disease. The described processes are useful for preparing compounds containing quaternary carbons, including structural analogs and derivatives of peloruside A.

专利号:US-8101779-B2
优先权日:2008-10-06
标题 :Enantioselective synthesis of (+) and (–)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene
发明人：CROOKS PETER A; VARTAK ASHISH PRAMOD
权利人:CROOKS PETER A; VARTAK ASHISH PRAMOD; UNIV KENTUCKY RES FOUND
摘要:Methods for the enantioselective synthesis of (+) and (−) lofexidine or 2-[1-(2,6)-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene involve converting (+) or (−) 1-methyl-1-[2,6-dichlorophenoxy]ethanamide to an (+) or (−) imino-ether intermediate by electrophilic attack of the amide oxygen by a trimethoxonium ion and, without isolation, converting the (+) or (−) imino-ether intermediate to (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene by adding ethylene diamine; and optionally converting the (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene into a pharmaceutically acceptable acid addition salt thereof.