4,4-Difluoro-L-prolinamide hydrochloride → (2S)-1-[6-(Cyclopropylmethoxy)-5-(1-hydroxycyclobutyl)pyridine-2-carbonyl]-4,4-difluoropyrrolidine-2-carboxamide

HRID 624990

반응식

HRID 624990 반응식
[CH:1]1([CH2:4][O:5][C:6]2[N:11]=[C:10]([C:12]([OH:14])=O)[CH:9]=[CH:8][C:7]=2[C:15]2([OH:19])[CH2:18][CH2:17][CH2:16]2)[CH2:3][CH2:2]1.Cl.[F:21][C:22]1([F:30])[CH2:26][NH:25][C@H:24]([C:27]([NH2:29])=[O:28])[CH2:23]1>>[CH:1]1([CH2:4][O:5][C:6]2[N:11]=[C:10]([C:12]([N:25]3[CH2:26][C:22]([F:30])([F:21])[CH2:23][C@H:24]3[C:27]([NH2:29])=[O:28])=[O:14])[CH:9]=[CH:8][C:7]=2[C:15]2([OH:19])[CH2:18][CH2:17][CH2:16]2)[CH2:2][CH2:3]1

참가 물질

3

반응물 2

HCID 451589094,4-Difluoro-L-prolinamide hydrochlorideHCID 710876116-Cyclopropylmethoxy-5-(1-hydroxy-cyclobutyl)-pyridine-2-carboxylic acid

생성물 1

HCID 76281331(2S)-1-[6-(Cyclopropylmethoxy)-5-(1-hydroxycyclobutyl)pyridine-2-carbonyl]-4,4-difluoropyrrolidine-2-carboxamide수율 26.6%

실험 절차

In analogy to the procedure described in Example 127 e), 6-(cyclopropylmethoxy)-5-(1-hydroxycyclobutyl)pyridine-2-carboxylic acid (CAN 1415899-53-4, 15 mg, 57 μmol) was reacted with (S)-4,4-difluoropyrrolidine-2-carboxamide hydrochloride (CAN 426844-51-1, 10.6 mg, 57 μmol) to give the title compound (6 mg, 21%) as light yellow oil, LC-MS (UV peak area, ESI) 100%, 396.1740 [MH+].

출처 및 근거

ORD 기록
ord-fc07b3a9ccd347fcb19d8361a8ca4171
출처 데이터셋
uspto-grants-2016_04
특허 번호
US09303012B2

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