Piperidin-4-ol → (3-(3,4-difluorophenyl)-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)(4-hydroxypiperidin-1-yl)methanone

関与物質

役割	名称	HCID	仕込み量
反応物	Piperidin-4-ol	HCID 79341	—
反応物	(S)-N-(3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl)-5-methyl-3-(2,4,5-trifluorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-1-carboxamide	HCID 46863441	—
反応物	tert-butyl 3-(3,4-difluorophenyl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridine-5(4H)-carboxylate	HCID 59345327	—
生成物	(3-(3,4-difluorophenyl)-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)(4-hydroxypiperidin-1-yl)methanone	HCID 46863445	—

反応手順

Compound 45 was prepared according to the procedure described for the synthesis of compound 37 by replacing intermediate 19 with intermediate 15, and replacing tert-leucine methyl amide with 4-hydroxypiperidine. 1H NMR (CDCl3) δ 7.46-7.51 (m, 1H), 7.32-7.36 (m, 1H), 7.20 (q, J=8.9 Hz, 1H), 3.96-4.08 (m, 3H), 3.60 (s, 2H), 3.41-3.47 (m, 2H), 3.08 (t, J=5.6 Hz, 2H), 2.78 (t, J=5.8 Hz, 2H), 2.54 (s, 3H), 1.97-2.01 (m, 2H), 1.63-1.72 (m, 2H). LCMS (+ESI) m/z=377 [M+H]+.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08653127B2
出典データセット	uspto-grants-2014_02
ORD ID	ord-a133a4d97b08442faec252ec27f4b685
出典メモ	uspto-grants-2014_02