Sodium triacetoxyborohydride → 2-{1-[4-(2-methyl-6-phenyl-[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)benzyl]-piperidin-4-yl}-3H-benzimidazole-5-carbonitrile

HRID 1851272노트

반응식

HRID 1851272 반응식
[CH3:1][C:2]1[N:24]=[C:5]2[N:6]=[C:7]([C:16]3[CH:23]=[CH:22][C:19]([CH:20]=O)=[CH:18][CH:17]=3)[C:8]([C:10]3[CH:15]=[CH:14][CH:13]=[CH:12][CH:11]=3)=[CH:9][N:4]2[N:3]=1.Cl.[NH:26]1[CH2:31][CH2:30][CH:29]([C:32]2[NH:33][C:34]3[CH:40]=[C:39]([C:41]#[N:42])[CH:38]=[CH:37][C:35]=3[N:36]=2)[CH2:28][CH2:27]1.[BH-](OC(C)=O)(OC(C)=O)OC(C)=O.[Na+]>>[CH3:1][C:2]1[N:24]=[C:5]2[N:6]=[C:7]([C:16]3[CH:23]=[CH:22][C:19]([CH2:20][N:26]4[CH2:27][CH2:28][CH:29]([C:32]5[NH:33][C:34]6[CH:40]=[C:39]([C:41]#[N:42])[CH:38]=[CH:37][C:35]=6[N:36]=5)[CH2:30][CH2:31]4)=[CH:18][CH:17]=3)[C:8]([C:10]3[CH:15]=[CH:14][CH:13]=[CH:12][CH:11]=3)=[CH:9][N:4]2[N:3]=1

참가 물질

4

반응물 3

HCID 5049666Sodium triacetoxyborohydrideHCID 687529322-Piperidin-4-yl-1h-benzoimidazole-5-carbonitrile hydrochloride saltHCID 866306814-(2-Methyl-6-phenyl[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)benzaldehyde

생성물 1

HCID 687509072-{1-[4-(2-methyl-6-phenyl-[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)benzyl]-piperidin-4-yl}-3H-benzimidazole-5-carbonitrile수율 36%

실험 절차

200 mg (0.64 mmol) 4-(2-methyl-6-phenyl[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)benzaldehyde and 200 mg (0.64 mmol) 2-piperidine-4-yl-3H-benzimidazole-5-carbonitrile hydrochloride salt were treated as described in example 2.0. Additional NaBH(OAc)3 has been added after 24 and 26 hours (two equivalents each). After five days stirring at room temperature the solvents have been evaporated and the residue was purified via chromatography. 121 mg of the desired compound were obtained.

후처리

  1. customhave been evaporated
  2. customthe residue was purified via chromatography

출처 및 근거

ORD 기록
ord-fe54f2e972ba4bc2baa2b8ba578f5b38
출처 데이터셋
uspto-grants-2015_02
특허 번호
US08957064B2

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