Diisopropylethylamine → (R)-1-(4-(4-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)propan-2-ol

참여 물질

역할	이름	HCID	투입량
반응물	Diisopropylethylamine	HCID 81531	—
반응물	(R)-1,2-Epoxypropane	HCID 146261	—
반응물	3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-5-(4-(piperazin-1-yl)phenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridinehydrochloride	HCID 90031507	—
용매	Ethanol	HCID 702	—
생성물	(R)-1-(4-(4-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)propan-2-ol	HCID 90030866	97.5%

반응 단계

Using similar reaction conditions as described in step-i of example-82A, 3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-5-(4-(piperazin-1-yl)phenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine hydrochloride (step 1 example 103) (150 mg. 0.606 mmol) was alkylated using (R)-2-methyloxirane (22 mg, 0.371 mmol), DIPEA (96 mg, 0.74 mmol) and ethanol (3 mL) to get 160 mg (97.5% yield) of the titled compound. MS: m/z=665.3 (M+1).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US09353107B2
출처 데이터셋	uspto-grants-2016_05
ORD ID	ord-262c47d2e67d43bcae9ece83e0700f53
출처 메모	uspto-grants-2016_05