CAS: 154598-52-4; (S)-6-Chloro-4-(Cyclopropylethynyl)-4-(Trifluoromethyl)-1H-Benzo[d][1,3]Oxazin-2(4H)-One

上下游产品

-3,1-benzoxazin-2-one(S)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-1-(4'-methoxyphenyl)methyl-3,1-benzoxazin-2-one phosgene (2S)-2-(2-amino-5-chlorophenyl)-4-cyclopropyl-1,1,1-trifluorobut-3-yn-2-ol 4-Nitrophenyl chloroformatepiperidine 8-Hydroxyefavirenz

1,4-二氯苯置于trans-N,N'-Dimethyl-1,2-Cyclohexyldiamine,Potassium Phosphate,Copper(L) Iodide,正丁基锂,Naphthalene-1-Sulfonic Acid ((R)-2-Hydroxy-1-Methyl-2,2-Diphenyl-Ethyl)-Amide,Dimethylzinc体系中,用 四氢呋喃,正己烷,正庚烷,乙酸乙酯,甲苯 用作溶剂,化学反应 68.5H,反应生成依法韦仑
参考文献: Dmp-266 By Cyclisation[fr] Dmp-266 Par Cyclisation
标题: Dmp-266 By Cyclisation[fr] Dmp-266 Par Cyclisation
摘要:揭示了一种制备hiv药物efavirenz(也称为dmp-266)的方法,从1,4-二氯苯和其中间体开始.

专利信息

专利号:US-6028237-A
优先权日:1996-12-16
标题:Synthesis of cyclopropylacetylene
发明人：PARSONS JR RODNEY LAWRENCE
权利人:DU PONT PHARM CO
摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

专利号:US-7205402-B2
优先权日:2004-09-02
标 题 :Synthesis of a benzoxazinone
发明人：VEMISHETTI PURUSHOTHAM; CHADWICK SCOTT T; COSTELLO CARRIE A; DESIKAN SRIDHAR; REIFF EMILY A
权利人:BRISTOL MYERS SQUIBB CO
摘要:The present invention provides novel methods for the synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (III) n nwhich is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

专利号:US-5698741-A
优先权日:1995-05-25
标题 :Asymmetric synthesis of (-)6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one
发明人：THOMPSON ANDREW S; CORLEY EDWARD G; GRABOWSKI EDWARD J J; YASUDA NOBUYOSHI
权利人:MERCK & CO INC
摘要:An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.

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-5932726-A
优先权日:1996-12-16
标 题 :Asymmetric synthesis of benzoxazinones
发明人：PIERCE MICHAEL ERNEST; CHOUDHURY ANUSUYA; PARSONS JR RODNEY LAWRENCE; RADESCA LILIAN ALICIA
权利人:DU PONT PHARM CO
摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

专利号:US-6040480-A
优先权日:1997-04-07
标题 :Asymmetric synthesis of benzoxazinones
发明人：PIERCE MICHAEL E; CHEN CHENG Y; CHOUDHURY ANUSUYA; RADESCA LILIAN A; TAN LUSHI; ZHAO DALIAN
权利人:DU PONT PHARM CO
摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.