Azetidine → 4-Azetidin-1-yl-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamide

HRID 29536

反応式

HRID 29536 の反応式
Br[C:2]1[CH:7]=[CH:6][C:5]([S:8]([NH:11][C:12]2[CH:17]=[CH:16][C:15]([Cl:18])=[CH:14][C:13]=2[C:19]([C:21]2[CH:26]=[CH:25][N:24]=[CH:23][CH:22]=2)=[O:20])(=[O:10])=[O:9])=[CH:4][CH:3]=1.O.[O-]P([O-])([O-])=O.[K+].[K+].[K+].C1(P(C2C=CC=CC=2)C2C=CC3C(=CC=CC=3)C=2C2C3C(=CC=CC=3)C=CC=2P(C2C=CC=CC=2)C2C=CC=CC=2)C=CC=CC=1.[NH:82]1[CH2:85][CH2:84][CH2:83]1>CN(C=O)C.[Pd]>[N:82]1([C:2]2[CH:7]=[CH:6][C:5]([S:8]([NH:11][C:12]3[CH:17]=[CH:16][C:15]([Cl:18])=[CH:14][C:13]=3[C:19]([C:21]3[CH:26]=[CH:25][N:24]=[CH:23][CH:22]=3)=[O:20])(=[O:10])=[O:9])=[CH:4][CH:3]=2)[CH2:85][CH2:84][CH2:83]1

参加物

7

反応物 4

HCID 10422AzetidineHCID 634876Binap, (A+-)-HCID 100725304-Bromo-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamideHCID 22031701Potassium phosphate, tribasic, monohydrate

生成物 1

HCID 597885724-Azetidin-1-yl-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamide

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 6228Dimethylformamide溶媒

実験手順

The title compound was prepared according to the general procedure for the synthesis of heterocyclyl and heteroaryl substituted phenylsulfonyl derivatives previously described, using 4-Bromo-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamide 0.3 g (0.66 mmol), potassium phosphate tribasic monohydrate 0.91 g (3.96 mmol), rac-2,2′-bis (diphenylphosphino)-1,1′-binaphthyl 0.12 g (0.198 mmol), azetidine 0.18 g (3.3 mmol) and Pd (dba)3 60 mg (0.066 mmol) in 3 ml DMF, followed by workup and HPLC purification.

後処理

  1. customfollowed by workup and HPLC purification

出典と根拠

ORDレコード
ord-2b520ac099e541fe8df3e3358a8dc94e
出典データセット
uspto-grants-2008_09
特許番号
US07420055B2

関連ノート

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