(R)-(+)-1-Boc-3-aminopyrrolidine → (R)-((S)-tetrahydrofuran-3-yl) 3-(2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)pyrrolidine-1-carboxylate

HRID 526915

反応式

HRID 526915 の反応式
[Cl:1][C:2]1[CH:3]=[C:4]2[C:10]([C:11]3[N:16]=[C:15]([NH:17][C@H:18]4[CH2:22][CH2:21][N:20](S(C)(=O)=O)[CH2:19]4)[C:14]([F:27])=[CH:13][N:12]=3)=[CH:9][NH:8][C:5]2=[N:6][CH:7]=1.N[C@@H]1CCN(C(OC(C)(C)C)=O)C1.[C:41](=O)([O:50][C@H:51]1[CH2:55][CH2:54][O:53][CH2:52]1)[O:42]N1C(=O)CCC1=O>>[Cl:1][C:2]1[CH:3]=[C:4]2[C:10]([C:11]3[N:16]=[C:15]([NH:17][C@@H:18]4[CH2:22][CH2:21][N:20]([C:41]([O:50][C@H:51]5[CH2:55][CH2:54][O:53][CH2:52]5)=[O:42])[CH2:19]4)[C:14]([F:27])=[CH:13][N:12]=3)=[CH:9][NH:8][C:5]2=[N:6][CH:7]=1

参加物

4

反応物 3

HCID 854070(R)-(+)-1-Boc-3-aminopyrrolidineHCID 11229944Carbonic Acid 2,5-Dioxopyrrolidin-1-yl (S)-Tetrahydrofuran-3-yl EsterHCID 68008525(S)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-(1-(methylsulfonyl)pyrrolidin-3-yl)pyrimidin-4-amine

生成物 1

HCID 68007886(R)-((S)-tetrahydrofuran-3-yl) 3-(2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)pyrrolidine-1-carboxylate収率 47%

実験手順

According to the procedure for compound 398 using (R)-tert-butyl 3-aminopyrrolidine-1-carboxylate and (S)-2,5-dioxopyrrolidin-1-yl tetrahydrofuran-3-yl carbonate afforded 19.8 mg (47% yield) of 424 as a solid.

出典と根拠

ORDレコード
ord-e39f8134e463413cbe90d9547f34e926
出典データセット
uspto-grants-2016_05
特許番号
US09345708B2

関連ノート

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