Hydrochloric Acid → 4-[(R)-aminophenylmethyl]-1-piperidinecarboxylic acid phenylmethyl ester

HRID 2070702노트

반응식

HRID 2070702 반응식
CC([S@]([NH:7][C@@H:8]([C:25]1[CH:30]=[CH:29][CH:28]=[CH:27][CH:26]=1)[CH:9]1[CH2:14][CH2:13][N:12]([C:15]([O:17][CH2:18][C:19]2[CH:24]=[CH:23][CH:22]=[CH:21][CH:20]=2)=[O:16])[CH2:11][CH2:10]1)=O)(C)C.CO.Cl>O1CCOCC1>[NH2:7][C@@H:8]([C:25]1[CH:26]=[CH:27][CH:28]=[CH:29][CH:30]=1)[CH:9]1[CH2:14][CH2:13][N:12]([C:15]([O:17][CH2:18][C:19]2[CH:20]=[CH:21][CH:22]=[CH:23][CH:24]=2)=[O:16])[CH2:11][CH2:10]1

참가 물질

5

반응물 3

HCID 313Hydrochloric AcidHCID 887MethanolHCID 866632334-[(R)-[[(R)-(1,1-Dimethylethyl)sulfinyl]amino]phenylmethyl]-1-piperidinecarboxylic acid, phenylmethyl ester

생성물 1

HCID 666897524-[(R)-aminophenylmethyl]-1-piperidinecarboxylic acid phenylmethyl ester수율 105.2%

시약·촉매·용매 1

HCID 312751,4-Dioxane용매

실험 절차

A mixture of 4-[(R)-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]phenylmethyl]-1-piperidinecarboxylic acid, phenylmethyl ester (0.59 g), methanol (5 mL) and hydrogen chloride in 1,4-dioxane (4M, 5 mL) was stirred at room temperature for 10 minutes then concentrated in vacuo. The residue was diluted in dichloromethane (2 mL) and triturated with diethyl ether to afford the subtitle compound as a solid (470 mg).

후처리

  1. concentrationthen concentrated in vacuo
  2. additionThe residue was diluted in dichloromethane (2 mL)
  3. customtriturated with diethyl ether

출처 및 근거

ORD 기록
ord-f38057028e1349529e9fce1c308fd08e
출처 데이터셋
uspto-grants-2012_10
특허 번호
US08299246B2

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