专利号:US-2001044540-A1 优先权日:2000-03-23 标 题:Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 发明人:PARSONS RODNEY L; DOROW ROBERTA L; DAVULCU AKIN H; FORTUNAK JOSEPH M; HARRIS GREGORY D; KAUFFMAN GOSS S; NUGENT WILLIAM A; RADESCA LILIAN A 摘要:This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
专利号:US-6555686-B2 优先权日:2000-03-23 标题:Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 发明人:PARSONS RODNEY L; DOROW ROBERTA L; DAVULCU AKIN H; FORTUNAK JOSEPH M; HARRIS GREGORY D; KAUFFMAN GOSS S; NUGENT WILLIAM A; RADESCA LILIAN A 权利人:BRISTOL MYERS SQUIBB PHARMA 摘要:This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
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-7217851-B1 优先权日:2004-03-31 标 题:Synthesis of butadiynes 发明人:SURI SURESH C; TINNIRELLO MICHAEL G 权利人:US AIR FORCE 摘要:Provided is a method for the synthesis of 1,4-dicyclopropyl-1,3-butadiyne from CPA. Such butadiyne is prepared by oxidative coupling of cyclopropyl acetylene (CPA) using catalytic amounts each of copper (I)chloride and tetrametylethylenediamine (TMEDA) in isopropanol under aerobic conditions. The resulting butadiyne can serve as a fuel or a fuel additive for combustion in engines propelling motor vehicles, marine vessels, aircraft, rockets and other vehicles.
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.