trans-3,4-Difluorocinnamic acid → 1-[(e)-3-(3,4-Difluoro-phenyl)-acryloyl]-4-(3-piperidin-1-yl-propyl)-[1,4]diazepan-5-one

HRID 1867412

反応式

HRID 1867412 の反応式
ClC1C=C(/C=C/C(N2CCC(=O)NCC2)=O)C=CC=1Cl.[F:21][C:22]1[CH:23]=[C:24]([CH:30]=[CH:31][C:32]=1[F:33])/[CH:25]=[CH:26]/[C:27]([OH:29])=O.Cl.Cl.[N:36]1([CH2:42][CH2:43][CH2:44][N:45]2[C:51](=[O:52])[CH2:50][CH2:49][NH:48][CH2:47][CH2:46]2)[CH2:41][CH2:40][CH2:39][CH2:38][CH2:37]1>>[F:21][C:22]1[CH:23]=[C:24](/[CH:25]=[CH:26]/[C:27]([N:48]2[CH2:49][CH2:50][C:51](=[O:52])[N:45]([CH2:44][CH2:43][CH2:42][N:36]3[CH2:37][CH2:38][CH2:39][CH2:40][CH2:41]3)[CH2:46][CH2:47]2)=[O:29])[CH:30]=[CH:31][C:32]=1[F:33]

参加物

4

反応物 3

HCID 2733300trans-3,4-Difluorocinnamic acidHCID 620449211-[(E)-3-(3,4-Dichloro-phenyl)-acryloyl]-[1,4]diazepan-5-oneHCID 670807474-(3-Piperidin-1-yl-propyl)-[1,4]diazepan-5-one dihydrochloride2 回

生成物 1

HCID 684349441-[(e)-3-(3,4-Difluoro-phenyl)-acryloyl]-4-(3-piperidin-1-yl-propyl)-[1,4]diazepan-5-one

実験手順

In analogy to the procedure described in intermediate 1A, (E)-3,4-difluorocinnamic acid and 4-(3-piperidin-1-yl-propyl)-[1,4]diazepan-5-one-dihydrochloride (intermediate 4B, suspended in CH2Cl2 with 4 equivalent of Et3N) gave after purification on catridges, Si-Amine, 70 ml, 20 g (EtOAc) the title compound as a white powder. MS: 406.2 (MH+).

後処理

  1. customgave
  2. customafter purification on catridges, Si-Amine, 70 ml, 20 g (EtOAc) the title compound as a white powder

出典と根拠

ORDレコード
ord-12012dab71db4d73a74ed26fc5bb68a6
出典データセット
uspto-grants-2009_12
特許番号
US07632829B2

関連ノート

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