专利号:US-11274081-B2 优先权日:2016-05-30 标 题:Process for the synthesis of ivacaftor 发明人:REDDY DUMBALA SRINIVASA; KULKARNI AMOL ARVIND; NATARAJAN VASUDEVAN; SHARMA MRITYUNJAY KESHAVPRASAD 权利人:COUNCIL SCIENT IND RES 摘要:The present disclosed an improved process for the synthesis of ivacaftor starting from indole acetic acid ester which can be performed in batch as well as continuous flow synthesis. The present invention further disclosed to a continuous process for the synthesis of compound of formula (II) or formula (III) from compound of formula (I) in continuous flow reactor.
专利号:US-4376207-A 优先权日:1980-08-18 标 题 :Chiral synthesis of amino sugars 发明人:USKOKOVIC MILAN R; WOVKULICH PETER M 权利人:HOFFMANN LA ROCHE 摘要:A simple and economic chiral synthesis of optically active methyl L-acosaminide and methyl L-daunosaminide from propenyl acetate, said methyl L-acosaminide and methyl L-daunosaminide being coupling agents for the production of known antitumor agents.
专利号:US-4324726-A 优先权日:1979-07-25 标题 :Chiral synthesis of amino sugars 发明人:USKOKOVIC MILAN R; WOVKULICH PETER M 权利人:HOFFMANN LA ROCHE 摘要:A simple and economic chiral synthesis of optically active methyl L-acosaminide and methyl L-daunosaminide from propenyl acetate, said methyl L-acosaminide and methyl L-daunosaminide being coupling agents for the production of known antitumor agents.
专利号:US-2025066296-A1 优先权日:2021-12-14 标题 :Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; PHADKE AVINASH; RAI U SANKAPPA; CHANDRAN PRABU 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
专利号:US-4414402-A 优先权日:1981-12-02 标 题:[2S-(2β,2S*, 3β)]-3-Aminotetrahydro-5-methoxy-α-methyl-2-furanmethanol, an intermediate in the chiral synthesis of amino sugars 发明人:USKOKOVIC MILAN R; WOVKULICH PETER M 权利人:HOFFMANN LA ROCHE 摘要:A simple and economic chiral synthesis of optically active methyl L-acosaminide and methyl L-daunosaminide from propenyl acetate, said methyl L-acosaminide and methyl L-daunosaminide being coupling agents for the production of known antitumor agents.
专利号:WO-2012100419-A1 优先权日:2011-01-26 标 题 :Process for synthesis of 3-(n,n-disubstituted-amino)-2- substituted acrylate 发明人:GU HAINING; LI XIAOLING; ZHANG PENGFEI; ZHANG XIKUN; CHEN LIANG 权利人:HANGZHOU GREAT FOREST BIOMEDICAL LTD; GU HAINING; LI XIAOLING; ZHANG PENGFEI; ZHANG XIKUN; CHEN LIANG 摘要:Disclosed is a process for synthesis of 3-(N,N-disubstituted-amino)-2-substituted acrylate, which comprises carrying out amine-substitution reaction and elimination reaction for 2-substituted formylacetate alkali metal salt represented by formula (III) and amine complex represented by formula (II) in organic solvent 1 to obtain 3-(N,N-disubstituted-amino)-2-substituted acrylate represented by formula (I). The process uses N,N-disubstituted amine and carbon dioxide, or a liquid complex obtained by N,N-disubstituted amine and carbon dioxide as raw material, thereby it doesn't produce a side product influencing environment. The process has the advantages of reacting simply and operating easily.
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 108. 摘要:Ishikawa, T., Science of Synthesis Knowledge Updates, (2012) 2, 321. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).