Diisopropylethylamine → 2-(4-Fluorophenyl)propionic acid

関与物質

役割	名称	HCID	仕込み量
反応物	Diisopropylethylamine	HCID 81531	—
反応物	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
反応物	propyl [(7R)-7-(methylamino)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]acetate	HCID 86655417	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	2-(4-Fluorophenyl)propionic acid	HCID 2723915	—

反応手順

(33 mg) and HATU (76 mg) were dissolved in DMF (1.3 mL). DIPEA (87 μL, 0.315 mmol) was added and the mixture was stirred for 1 min before the addition of propyl [(7R)-7-(methylamino)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]acetate (50 mg) in 1 mL DMF. The reaction mixture was stirred for 2 h. The solvent was removed under vacuum and the residue was purified on silica gel (ethyl acetate/hexanes). The resulting diastereoisomers were separated on a Chiralpak AD column (20% iPrOH/Hexanes, 0.25% HCOOH). The propyl esters were hydrolysed to their corresponding acids using a procedure analogous to the one described in Step 2. MS (+ESI) m/z: 409.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08637671B2
出典データセット	uspto-grants-2014_01
ORD ID	ord-2e430c3310ff4cfc95166c1f0f1e9cc4
出典メモ	uspto-grants-2014_01