N-Methylphenylethanolamine → 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(3-{[(2-hydroxy-2-phenylethyl)-(methyl)amino]methyl}phenyl)-1H-indole-7-carboxamide

HRID 562043

반응식

HRID 562043 반응식
[CH2:1]([S:3]([N:6]1[CH2:11][CH2:10][CH:9]([C:12]2[C:20]3[C:15](=[C:16]([C:29]([NH2:31])=[O:30])[CH:17]=[C:18]([C:21]4[CH:26]=[CH:25][CH:24]=[C:23](C=O)[CH:22]=4)[CH:19]=3)[NH:14][CH:13]=2)[CH2:8][CH2:7]1)(=[O:5])=[O:4])[CH3:2].[CH3:32][NH:33][CH2:34][CH:35]([C:37]1[CH:42]=[CH:41][CH:40]=[CH:39][CH:38]=1)[OH:36].[BH-](OC(C)=O)(OC(C)=O)O[C:45](C)=O.[Na+]>>[CH2:1]([S:3]([N:6]1[CH2:7][CH2:8][CH:9]([C:12]2[C:20]3[C:15](=[C:16]([C:29]([NH2:31])=[O:30])[CH:17]=[C:18]([C:21]4[CH:26]=[CH:25][CH:24]=[C:23]([CH2:32][N:33]([CH2:34][CH:35]([OH:36])[C:37]5[CH:42]=[CH:41][CH:40]=[CH:39][CH:38]=5)[CH3:45])[CH:22]=4)[CH:19]=3)[NH:14][CH:13]=2)[CH2:10][CH2:11]1)(=[O:5])=[O:4])[CH3:2]

참가 물질

4

반응물 3

HCID 913N-MethylphenylethanolamineHCID 5049666Sodium triacetoxyborohydrideHCID 577328043-[1-(ethylsulfonyl)-4-piperidinyl]-5-(3-formylphenyl)-1H-indole-7-carboxamide

생성물 1

HCID 160381073-[1-(ethylsulfonyl)-4-piperidinyl]-5-(3-{[(2-hydroxy-2-phenylethyl)-(methyl)amino]methyl}phenyl)-1H-indole-7-carboxamide수율 36.6%

실험 절차

Following the general procedure of example 1, 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(3-formylphenyl)-1H-indole-7-carboxamide (50.0 mg, 0.112 mmol), 2-(methylamino)-1-phenylethanol (129.9 mg, 0.86 mmol) and NaBH(OAc)3 (58.0 mg, 0.303 mmol) were reacted to give the title compound (22.1 mg, 36.6%).

후처리

  1. customwere reacted

출처 및 근거

ORD 기록
ord-aae99d0ad98b4b5092048af517f4721f
출처 데이터셋
uspto-grants-2011_11
특허 번호
US08063071B2

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