2-Thiopheneboronic acid → N-[2-(2-chloro-5-(2-thienyl)pyrimidine-4-ylamino)ethyl]acetamide

반응식

[Cl:1][C:2]1[N:7]=[C:6]([NH:8][CH2:9][CH2:10][NH:11][C:12](=[O:14])[CH3:13])[C:5](I)=[CH:4][N:3]=1.[S:16]1[CH:20]=[CH:19][CH:18]=[C:17]1B(O)O>>[Cl:1][C:2]1[N:7]=[C:6]([NH:8][CH2:9][CH2:10][NH:11][C:12](=[O:14])[CH3:13])[C:5]([C:17]2[S:16][CH:20]=[CH:19][CH:18]=2)=[CH:4][N:3]=1

참가 물질

반응물 2

HCID 27339602-Thiopheneboronic acid

HCID 59550867N-[2-(2-chloro-5-iodopyrimidine-4-ylamino)ethyl]acetamide

생성물 1

HCID 58985576N-[2-(2-chloro-5-(2-thienyl)pyrimidine-4-ylamino)ethyl]acetamide수율 79%

실험 절차

In the reaction of N-[2-(2-chloro-5-iodopyrimidine-4-ylamino)ethyl]-acetamide (870 mg, 2.6 mmol) with thiophen-2-boronic acid (359 mg, 2.8 mmol) according to procedure 3, the desired product is obtained in 79% yield (602 mg) after chromatographic purification (silica gel, ethyl acetate/hexane (0%-90% ethyl acetate)).

출처 및 근거

ORD 기록: ord-29605186a2a8437da7a89550d431531b
출처 데이터셋: uspto-grants-2010_11
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US07825128B2

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