4-Iodobenzyl alcohol → 2-{4-[3-(4-Hydroxymethyl-phenyl)-prop-2-ynyloxy]-phenoxymethyl}-pyrrolidine-1-carboxylic acid tert-butyl ester

HRID 12927

반응식

HRID 12927 반응식
[C:1]([O:5][C:6]([N:8]1[CH2:12][CH2:11][CH2:10][CH:9]1[CH2:13][O:14][C:15]1[CH:20]=[CH:19][C:18]([O:21][CH2:22][C:23]#[CH:24])=[CH:17][CH:16]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].I[C:26]1[CH:33]=[CH:32][C:29]([CH2:30][OH:31])=[CH:28][CH:27]=1.N1CCCC1>Cl[Pd]Cl.O>[C:1]([O:5][C:6]([N:8]1[CH2:12][CH2:11][CH2:10][CH:9]1[CH2:13][O:14][C:15]1[CH:20]=[CH:19][C:18]([O:21][CH2:22][C:23]#[C:24][C:26]2[CH:33]=[CH:32][C:29]([CH2:30][OH:31])=[CH:28][CH:27]=2)=[CH:17][CH:16]=1)=[O:7])([CH3:3])([CH3:2])[CH3:4]

참가 물질

6

반응물 3

HCID 290124-Iodobenzyl alcoholHCID 31268PyrrolidineHCID 866196562-(4-Prop-2-ynyloxy-phenoxymethyl)-pyrrolidine-1-carboxylic acid tert-butyl ester

생성물 1

HCID 684297222-{4-[3-(4-Hydroxymethyl-phenyl)-prop-2-ynyloxy]-phenoxymethyl}-pyrrolidine-1-carboxylic acid tert-butyl ester수율 20.5%

시약·촉매·용매 2

HCID 24290Palladium Chloride촉매HCID 962Water용매

실험 절차

General procedure A was followed using the product from step 3 Example 1 (266 mg, 1.0546 mmol), p-iodobenzylalcohol (156.5 mg, 0.669 mmol), PdCl2 (2.5 mg, 0.014 mmol), pyrrolidine (0.277 mL, 3.34 mmol), water (0.844 mL) to give the title compound (60 mg, 20.5%).

출처 및 근거

ORD 기록
ord-98f3564561be419fbc072cf9e881ed13
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07728032B2

연결된 노트

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