专利号:US-8957204-B2 优先权日:2010-10-14 标题 :Process for the synthesis of cyclic carbamates 发明人:BRENNER MEINRAD; CARREIRA ERICK M; CHINKOV NICKA; LORENZI MIRIAM; WARM ALEKSANDER; ZIMMERMANN LOTHAR 权利人:BRENNER MEINRAD; CARREIRA ERICK M; CHINKOV NICKA; LORENZI MIRIAM; WARM ALEKSANDER; ZIMMERMANN LOTHAR; LONZA AG 摘要:The invention is directed to a process for the preparation of a cyclic carbamate starting with a chiral propargylic alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C 2-5 -alkyl C 2-5 -carboxylates and mixtures of at least one C 2-5 -alkyl C 2-5 -carboxylate with at least one C 5-8 -alkane. Another aspect of the invention is directed to a process for the synthesis of said cyclic carbamate starting described above, wherein also a process for the preparation of the chiral propargylic alcohol is provided.
专利号:US-8283502-B2 优先权日:2009-04-09 标题:Autocatalytic process for the synthesis of chiral propargylic alcohols 发明人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK 权利人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK; LONZA AG 摘要:An autocatalytic process for the synthesis of chiral propargylic alcohols.
专利号:US-8115032-B2 优先权日:2009-04-09 标 题 :Process for the synthesis of a propargylic alcohol 发明人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK 权利人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK; LONZA AG 摘要:A process for the preparation of the compound of formula
专利号:US-8969550-B2 优先权日:2010-10-14 标 题 :Process for the synthesis of cyclic carbamates 发明人:BRENNER MEINRAD; CARREIRA ERICK M; CHINKOV NICKA; LORENZI MIRIAM; WARM ALEKSANDER; ZIMMERMANN LOTHAR 权利人:BRENNER MEINRAD; CARREIRA ERICK M; CHINKOV NICKA; LORENZI MIRIAM; WARM ALEKSANDER; ZIMMERMANN LOTHAR; LONZA AG 摘要:The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C 2-5 -alkyl C 2-5 -carboxylates and mixtures of at least one C 2-5 -alkyl C 2-5 -carboxylate with at least one C 5-8 -alkane.
专利号:WO-2011000532-A2 优先权日:2009-07-03 标题:Method for the enantioselective addition of organometallic carbon nucleophiles to trifluoromethyl ketones and use of the method in the synthesis of hiv reverse transcriptase inhibitors
专利号:US-6015926-A 优先权日:1997-05-16 标题 :Efficient enantioselective addition reaction using an organozinc reagent 发明人:CHEN CHENG YI; TAN LUSHI; TILLYER RICHARD D 权利人:MERCK & CO INC 摘要:An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.