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HRID 580592作成日:2026年10月26日

8,9-Difluoro-3-methyl-6-oxo-2,3-dihydro-6H-1-oxa-3a-aza-phenalene-5-carboxylic acid → 10-(cis-3-t-Butoxycarbonylamino-4-methyl-1-pyrrolidinyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid

https://huagongshe.com/reaction/580592

反応式

関与物質

役割名称HCID仕込み量
反応物8,9-Difluoro-3-methyl-6-oxo-2,3-dihydro-6H-1-oxa-3a-aza-phenalene-5-carboxylic acidHCID 534278—
反応物(3S,4S)-3-(Boc-amino)-4-methylpyrrolidineHCID 11138119—
溶媒Dimethyl SulfoxideHCID 679—
生成物10-(cis-3-t-Butoxycarbonylamino-4-methyl-1-pyrrolidinyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acidHCID 7041939770.7%

反応手順

A mixture of 9,10-difluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid (0.5 g), anhydrous dimethyl sulfoxide (10 ml) and cis-3-t-butoxycarbonylamino-4-methylpyrrolidine (0.54 g) was stirred for 2 hours at 90°-100° C. and then concentrated. To the residue was added methanol and the resulting precipitate was collected by filtration and then washed with cold methanol to give the title compound (0.58 g) as yellowish powder, mp 219°-220° C.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US04753953
出典データセットuspto-grants-1988_06
ORD IDord-b7f2201273df4e4fa8288ce078d6c38d
出典メモuspto-grants-1988_06