Ammonium formate → tert-Butyl cis(+/-)-4-amino-3-(2,2-difluoropropoxy)piperidine-1-carboxylate

HRID 43712ノート

反応式

HRID 43712 の反応式
C([N:8](C(OCC1C=CC=CC=1)=O)[C@H:9]1[CH2:14][CH2:13][N:12]([C:15]([O:17][C:18]([CH3:21])([CH3:20])[CH3:19])=[O:16])[CH2:11][C@H:10]1[O:22][CH2:23][C:24]([F:27])([F:26])[CH3:25])C1C=CC=CC=1.C([O-])=O.[NH4+]>[Pd].CO>[NH2:8][C@H:9]1[CH2:14][CH2:13][N:12]([C:15]([O:17][C:18]([CH3:19])([CH3:20])[CH3:21])=[O:16])[CH2:11][C@H:10]1[O:22][CH2:23][C:24]([F:27])([F:26])[CH3:25]

参加物

5

反応物 2

HCID 2723923Ammonium formateHCID 86648657tert-Butyl cis(+/-)-4-{benzyl[(benzyloxy)carbonyl]amino}-3-(2,2-difluoropropoxy)piperidine-1-carboxylate

生成物 1

HCID 86648656tert-Butyl cis(+/-)-4-amino-3-(2,2-difluoropropoxy)piperidine-1-carboxylate収率 93.8%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 887Methanol溶媒

実験手順

The same operation as in Example (90d) was performed using tert-butyl cis(±)-4-{benzyl[(benzyloxy)carbonyl]amino}-3-(2,2-difluoropropoxy)piperidine-1-carboxylate obtained in Example (128c) (1.31 g, 2.5 mmol), 10% Pd/C (wet, 0.4 g), ammonium formate (0.95 g, 15 mmol) and methanol (20 mL), to obtain 0.69 g of the title compound as a colorless oily substance (64%).

出典と根拠

ORDレコード
ord-0938eb97bbe545139357a9812cde5ea2
出典データセット
uspto-grants-2013_09
特許番号
US08536197B2

反応ノート

読み込み中…