Diisopropylethylamine → HCID 59486429、化合物

DIPEA (2.5 eq.), HOAt (1.0 eq.) and EDCl (1.5 eq.) were added to a solution of 2-(2-(6-methoxynaphthalen-2-ylsulfonyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-1-yl)-acetic acid S2 (0.195 mmol, 1.0 eq.) in DCM (3 ml) at 0° C. and the mixture was stirred for 15 min at RT. Then (R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydro-naphthalen-1-amine A6 (0.234 mmol, 1.2 eq.) in DCM (2 ml) was added at 0° C. and the mixture was stirred overnight at RT. The reaction mixture was diluted with DCM and extracted with aqueous NaHCO3 solution, aqueous NH4Cl solution, water and saturated NaCl solution. The organic phase was dried (Na2SO4), concentrated to small volume and purified by column chromatography (alox). Yield: 55%; m/z=627.4 [MH]+

1. extractionextracted with aqueous NaHCO3 solution, aqueous NH4Cl solution, water and saturated NaCl solution
2. dry with materialThe organic phase was dried (Na2SO4)
3. concentrationconcentrated to small volume
4. custompurified by column chromatography (alox)

ORDレコード

ord-4ddd0ebc53af424aae12e33090d26fac

出典データセット

uspto-grants-2012_04

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08158628B2