4-(Bromomethyl)benzenesulfonyl chloride → (RS)-2-(4-Fluoro-phenyl)-1-(4-methoxymethyl-benzenesulfonyl)-pyrrolidine

HRID 1594765ノート

反応式

HRID 1594765 の反応式
[F:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]2[CH2:12][CH2:11][CH2:10][N:9]2[S:13]([C:16]2[CH:21]=[CH:20][C:19]([CH2:22]Cl)=[CH:18][CH:17]=2)(=[O:15])=[O:14])=[CH:4][CH:3]=1.FC1C=CC(C2CCCN2)=CC=1.BrCC1C=CC(S(Cl)(=O)=O)=CC=1.[CH3:48][O-:49].[Na+]>CO>[F:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]2[CH2:12][CH2:11][CH2:10][N:9]2[S:13]([C:16]2[CH:21]=[CH:20][C:19]([CH2:22][O:49][CH3:48])=[CH:18][CH:17]=2)(=[O:15])=[O:14])=[CH:4][CH:3]=1

参加物

6

反応物 4

HCID 27344094-(Bromomethyl)benzenesulfonyl chlorideHCID 38655602-(4-Fluorophenyl)pyrrolidineHCID 10942334Sodium MethoxideHCID 21706775(RS)-2-(4-fluoro-phenyl)-1-(4-chloromethyl-benzenesulfonyl)-pyrrolidine

生成物 1

HCID 21706731(RS)-2-(4-Fluoro-phenyl)-1-(4-methoxymethyl-benzenesulfonyl)-pyrrolidine

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

実験手順

Reaction of (RS)-2-(4-fluoro-phenyl)-1-(4-chloromethyl-benzenesulfonyl)-pyrrolidine (0.50 g, 1.41 mmol), which was prepared in accordance with the general method of example 1e from (RS)-2-(4-fluoro-phenyl)-pyrrolidine and 4-bromomethyl-benzenesulfonyl chloride, with sodium methanolate in MeOH for 80 h at 50° C. yielded after crystallization from EE/hexane 0.28 g (52%) of the title compound as a white solid, m.p. 115° C., and MS: m/e=349 (M+).

後処理

  1. customyielded
  2. customafter crystallization from EE/hexane 0.28 g (52%) of the title compound as a white solid, m.p. 115° C., and MS

出典と根拠

ORDレコード
ord-ba6233d6c9034b0db398517187b81c97
出典データセット
uspto-grants-2001_09
特許番号
US06284785B1

反応ノート

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