专利号:US-12043612-B2 优先权日:2020-05-09 标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same 发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY 权利人:ARVINAS OPERATIONS INC 摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:US-4235807-A 优先权日:1979-07-02 标 题:Synthesis of 2,6-disubstituted benzonitriles 发明人:FUHLHAGE DONALD W 权利人:THOMPSON HAYWARD CHEMICAL 摘要:A one step method of converting 2,6-disubstituted benzaldehydes to 2,6-disubstituted benzonitriles which comprises heating benzaldehyde in the presence of a hydroxylamine and a dehydrating agent for about 1 to 40 hours at a temperature of 110°-250° and then separating out the resultant 2,6-disubstituted benzonitrile.
专利号:US-4536599-A 优先权日:1978-08-22 标题:Synthesis of amine derivatives 发明人:MASUKO FUJIO; KATSURA TADASHI 权利人:SUMITOMO CHEMICAL CO 摘要:An amine of the formula, ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are each hydrogen, alkyl or the like and n is 1, 2 or 3, including α-phenyl-β-(p-tolyl)-ethylamine, which is useful as an optically resolving agent, an intermediate of medicines and the like, is effectively produced by a novel process comprising hydrolysis of the corresponding nitrile of the formula, ##STR2## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above, followed by alkali-decomposition of the resulting amide of the formula, ##STR3## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above. An amide including the above one is effectively produced by hydrolysis of the corresponding nitrile in the presence of a base and hydrogen peroxide using an organic quaternary ammonium salt and/or a tertiary amine as a catalyst.
专利号:US-6960601-B2 优先权日:2001-09-24 标题 :Preparation and use of imidazole derivatives for treatment of obesity 发明人:SMITH ROGER A; O'CONNOR STEPHEN J; WIRTZ STEPHAN-NICHOLAS; WONG WAI C; CHOI SOONGYU; KLUENDER HAROLD C E; SU NING; WANG GAN; ACHEBE FURAHI; YING SHIHONG 权利人:BAYER PHARMACEUTICALS CORP 摘要:This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:CN-108752217-A 优先权日:2018-07-18 标题:A new method for the synthesis of dolutegravir key intermediate 2,4-difluorobenzylamine
专利号:EP-0040896-B1 优先权日:1978-08-22 标题:Synthesis of amides