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HRID 403260作成日:2026年10月26日

5-Fluoro-3-pyridinamine → (R)-6,6-difluoro-5-(2-fluoro-5-(5-fluoropyridin-3-ylamino)phenyl)-5,7,7-trimethyl-1,4-oxazepan-3-one

https://huagongshe.com/reaction/403260

反応式

関与物質

役割名称HCID仕込み量
反応物5-Fluoro-3-pyridinamineHCID 574450—
反応物(R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepan-3-oneHCID 58562968—
生成物(R)-6,6-difluoro-5-(2-fluoro-5-(5-fluoropyridin-3-ylamino)phenyl)-5,7,7-trimethyl-1,4-oxazepan-3-oneHCID 6822717526%

反応手順

Prepared in an analogous manner as described for intermediate A9A or A13A from (R)-5-(5-bromo-2-fluorophenyl)-6,6-difluoro-5,7,7-trimethyl-1,4-oxazepan-3-one (intermediate A16B) (200 mg, 546 μmol) and commercially available 3-amino-5-fluoropyridine [CAS no 210169-05-4] (122 mg, 1.09 mmol). The (R)-6,6-difluoro-5-(2-fluoro-5-(5-fluoropyridin-3-ylamino)phenyl)-5,7,7-trimethyl-1,4-oxazepan-3-one (56 mg, 26%) was obtained as an off-white foam. MS (ISP): m/z=398.2 [(M+H)+].

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08748418B2
出典データセットuspto-grants-2014_06
ORD IDord-db8bbf54e5174e408e2140a1fa0cffc6
出典メモuspto-grants-2014_06