1-(p-Tolyl)piperazine → [(2S,4S)-1-Benzyl-4-(2,4-difluoro-benzylamino)-pyrrolidin-2-yl]-(4-p-tolyl-piperazin-1-yl)-methanone

HRID 490616

反応式

HRID 490616 の反応式
[CH2:1]([N:8]1[CH2:12][CH:11]([N:13](C(OC(C)(C)C)=O)[CH2:14][C:15]2[CH:20]=[CH:19][C:18]([F:21])=[CH:17][C:16]=2[F:22])[CH2:10][CH:9]1[C:30](O)=[O:31])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[C:33]1([CH3:45])[CH:38]=[CH:37][C:36]([N:39]2[CH2:44][CH2:43][NH:42][CH2:41][CH2:40]2)=[CH:35][CH:34]=1>>[CH2:1]([N:8]1[CH2:12][C@@H:11]([NH:13][CH2:14][C:15]2[CH:20]=[CH:19][C:18]([F:21])=[CH:17][C:16]=2[F:22])[CH2:10][C@H:9]1[C:30]([N:42]1[CH2:41][CH2:40][N:39]([C:36]2[CH:35]=[CH:34][C:33]([CH3:45])=[CH:38][CH:37]=2)[CH2:44][CH2:43]1)=[O:31])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1

参加物

3

反応物 2

HCID 831131-(p-Tolyl)piperazineHCID 675474701-Benzyl-4-[tert-butoxycarbonyl-(2,4-difluoro-benzyl)-amino]-pyrrolidine-2-carboxylic acid

生成物 1

HCID 67548059[(2S,4S)-1-Benzyl-4-(2,4-difluoro-benzylamino)-pyrrolidin-2-yl]-(4-p-tolyl-piperazin-1-yl)-methanone収率 2.6%

実験手順

As described for Example 1f, 1-benzyl-4-[tert-butoxycarbonyl-(2,4-difluoro-benzyl)-amino]-pyrrolidine-2-carboxylic acid (60.0 mg, 0.134 mmol) was converted, using 1-p-tolyl-piperazine instead of 2-piperazin-1-yl-benzonitrile, to the title compound (1.8 mg, 2.6%) as light yellow oil. MS m/e=505.4 [M+H]+.

出典と根拠

ORDレコード
ord-fc184cf34c5a48b98b4a5c850e9cd027
出典データセット
uspto-grants-2009_05
特許番号
US07528136B2

関連ノート

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