Triethylamine → Cis(+/-)2-[4-(dibenzylamino)-3-methoxypiperidin-1-yl]ethyl methanesulfonate

HRID 255335노트

반응식

HRID 255335 반응식
[CH2:1]([N:8]([CH2:20][C:21]1[CH:26]=[CH:25][CH:24]=[CH:23][CH:22]=1)[C@H:9]1[CH2:14][CH2:13][N:12]([CH2:15][CH2:16][OH:17])[CH2:11][C@H:10]1[O:18][CH3:19])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[CH3:27][S:28](Cl)(=[O:30])=[O:29].C(N(CC)CC)C.CS(OCCN1CCC(NC(OC(C)(C)C)=O)CC1)(=O)=O>>[CH3:27][S:28]([O:17][CH2:16][CH2:15][N:12]1[CH2:13][CH2:14][C@H:9]([N:8]([CH2:1][C:2]2[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=2)[CH2:20][C:21]2[CH:22]=[CH:23][CH:24]=[CH:25][CH:26]=2)[C@H:10]([O:18][CH3:19])[CH2:11]1)(=[O:30])=[O:29]

참가 물질

5

반응물 4

HCID 8471TriethylamineHCID 31297Methanesulfonyl chlorideHCID 568344782-(4-((Tert-butoxycarbonyl)amino)piperidin-1-yl)ethyl methanesulfonateHCID 602017752-[(3R,4S)-4-(Dibenzylamino)-3-methoxypiperidin-1-yl]ethanol2회

생성물 1

HCID 86642652Cis(+/-)2-[4-(dibenzylamino)-3-methoxypiperidin-1-yl]ethyl methanesulfonate

실험 절차

Cis(±)2-[4-(dibenzylamino)-3-methoxypiperidin-1-yl]ethanol (Intermediate 170, 740 mg, 2.1 mmol) was reacted with methanesulfonyl chloride (0.20 mL, 2.5 mmol) in the presence of triethylamine (0.41 mL, 2.9 mmol) as described for Intermediate 6. The crude product was presumed to be unstable and was used without further purification directly for the next step.

후처리

  1. customwas used without further purification directly for the next step

출처 및 근거

ORD 기록
ord-468b698ae07d44469d91b90c7f81bb0b
출처 데이터셋
uspto-grants-2011_01
특허 번호
US07875715B2

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