专利号:US-5618944-A 优先权日:1993-05-05 标题:Method for the synthesis of anthrapyrazolones 发明人:ZHANG LIN-HUA; AUERBACH JOSEPH 权利人:DU PONT MERCK PHARMA 摘要:This invention relates to compounds, including 5-chloro-2-[2-[[(4-methylphenyl)sulfonyl]oxy]ethyl]-7-[2,4,6-trimethylphenyl)methoxy]anthra[1,9-cd]pyrazol-6(2H)-one and analogs thereof, which are useful as intermediates for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone. This invention also relates to methods for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone.
专利号:US-6288297-B1 优先权日:1998-10-01 标 题:Process for the preparation of cyclopropylacetylene 发明人:WANG ZHE; YIN JIANGUO; FORTUNAK JOSEPH M; CAMPAGNA SILVIO 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn is hydroxy protected to form 1,1,1-trichloro-2-cyclopropylethyltosylate; which in turn undergoes elimination to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.
专利号:US-6359164-B1 优先权日:1998-10-01 标 题:Process for the preparation of cyclopropylacetylene 发明人:WANG ZHE; FORTUNAK JOSEPH M 摘要:The present invention relates generally to novel methods for the preparation of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor with superior anti-retroviral activity. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn undergoes elimination to form 1,1-dichloro-2-cyclopropyl-ethene; which in turn undergoes elimination to form cyclopropyl acetylene.
专利号:EP-0700390-A1 优先权日:1993-05-05 标 题 :Intermediates and methods for the synthesis of anthrapyrazolone anticancer agents
专利号:DD-286172-A5 优先权日:1989-07-12 标 题:PROCESS FOR SYNTHESIS OF SULFONATES OF 6-HYDROXY-2H-CHROMEN-2-ONE
专利号:WO-9425441-A1 优先权日:1993-05-05 标 题:Intermediates and methods for the synthesis of anthrapyrazolone anticancer agents