专利号:US-6395898-B1 优先权日:2000-06-09 标 题:Trans-glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine 发明人:MCNAMARA JAMES M; ZHAO MATTHEW M 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
专利号:US-6130331-A 优先权日:1998-09-11 标题 :Chemical synthesis of a chiral 1,4-oxazin-2-one 发明人:ASHWOOD MICHAEL STEWART; COTTRELL IAN FRANK; BISHOPS BRIAN CHRISTOPHER; EDWARDS JOHN SIMON 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a process for the preparation of substantially pure N-((S)-(-)-α-methylbenzyl)-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one hydrochloride, which comprises selectively crystallising the (S,S)-diastereomer as the hydrochloride salt from a mixture of the (S,R)- and (S,S)-diastereomers in an organic solvent, and collecting the resultant crystalline product.
专利号:US-6046325-A 优先权日:1998-09-11 标 题:Chemical synthesis of 1,4-oxazin-2-ones 发明人:ASHWOOD MICHAEL STEWART; BISHOP BRIAN CHRISTOPHER; COTTRELL IAN FRANK 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R 1 is a C 1-6 alkyl or arylC 1-4 alkyl group; and R 2 is a hydrogen atom, a halogen atom, or a group selected from C 1-6 alkyl, CF 3 or C 1-6 alkoxy substituted by C 1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.
专利号:GB-2341387-A 优先权日:1998-09-11 标题 :Synthesis of a chiral 1,4-oxazin-2-one derivative
专利号:US-2002022725-A1 优先权日:2000-06-09 标 题 :Trans-glycosidation process for the synthesis of (2R, 2-alpha-R, 3a) -2-(1- (3,5-bis(trifluoromethyl) phenyl) ethoxy ) -3- (4-fluorophenyl) -1, 4-oxazine
专利号:WO-0196319-A1 优先权日:2000-06-09 标题 :Trans-glycosidation process for the synthesis of (2r, 2-alpha-r, 3a)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
参考文献:10.1134/s1063774518030045 摘要:Kumar B, Battini N, Ahmed QN, Ali A, Gupta VK. X-Ray Study of 7a-(2-Chlorophenyl)-7a,8a,9,10,11,12ahexadronaptho[ 1',2':4,5]furo[3,2-d]pyrrolo[2,1-b]oxazole and 2-(4-fluorophenyl)-2-hydroxynaptho[2,1-b]furan-1(2H)-one. Crystallography Reports. 2018 May;63(3):382–7. doi: 10.1134/s1063774518030045.