4-Piperidinamine → 3-[2-(4-amino-1-piperidinyl)-8-(2,6-difluorophenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-4-yl]-N-cyclopropyl-4-methylbenzamide

HRID 222958

反応式

HRID 222958 の反応式
[CH:1]1([NH:4][C:5](=[O:36])[C:6]2[CH:11]=[CH:10][C:9]([CH3:12])=[C:8]([C:13]3[C:14]4[CH:26]=[CH:25][C:24](=[O:27])[N:23]([C:28]5[C:33]([F:34])=[CH:32][CH:31]=[CH:30][C:29]=5[F:35])[C:15]=4[N:16]=[C:17](S(C)(=O)=O)[N:18]=3)[CH:7]=2)[CH2:3][CH2:2]1.[NH:37]1[CH2:42][CH2:41][CH:40]([NH2:43])[CH2:39][CH2:38]1>>[NH2:43][CH:40]1[CH2:41][CH2:42][N:37]([C:17]2[N:18]=[C:13]([C:8]3[CH:7]=[C:6]([CH:11]=[CH:10][C:9]=3[CH3:12])[C:5]([NH:4][CH:1]3[CH2:3][CH2:2]3)=[O:36])[C:14]3[CH:26]=[CH:25][C:24](=[O:27])[N:23]([C:28]4[C:33]([F:34])=[CH:32][CH:31]=[CH:30][C:29]=4[F:35])[C:15]=3[N:16]=2)[CH2:38][CH2:39]1

参加物

3

反応物 2

HCID 4243614-PiperidinamineHCID 57434545N-cyclopropyl-3-[8-(2,6-difluorophenyl)-2-(methylsulfonyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-4-yl]-4-methylbenzamide

生成物 1

HCID 119478993-[2-(4-amino-1-piperidinyl)-8-(2,6-difluorophenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-4-yl]-N-cyclopropyl-4-methylbenzamide

実験手順

The title compound is prepared from compound N-cyclopropyl-3-[8-(2,6-difluorophenyl)-2-(methylsulfonyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-4-yl]-4-methylbenzamide and 4-piperidinamine by following the General Procedure for Sulfoxide/Sulfone/Sulfone Displacement, as disclosed above. The concentrated reaction mixture is precipitated with ethyl acetate/hexanes, and filtered. The desired product is obtained as a yellow solid (75 mg, 100%) 94% pure by HPLC: LC-MS m/z 531 (M+H)+, 1.65 min (ret time).

後処理

  1. customThe concentrated reaction mixture
  2. customis precipitated with ethyl acetate/hexanes
  3. filtrationfiltered

出典と根拠

ORDレコード
ord-551892f2382541c2a7625af1536d1058
出典データセット
uspto-grants-2012_06
特許番号
US08207176B2

関連ノート

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