Diisopropylethylamine → N-((1R,2S)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)propan-2-yl)cyclopropanesulfonamide

(1R,2S)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)propan-2-amine (43a, 102 mg, 0.24 mmol) and DIPEA (170 μL, 0.97 mmol) was dissolved in NMP (2 mL). cyclopropanesulfonyl chloride (40 μL, 0.39 mmol) was added and the reaction mixture was stirred at room temperature for 1 hour. The reaction mixture was diluted with water (10 mL) and extracted with EtOAc (2×10 mL), the organic phase was washed with brine, dried (Na2SO4), filtered and evaporated to give an oily residue (NMP residues). The crude material was further purified by HPLC. Yield 80 mg (62%)

1. extractionextracted with EtOAc (2×10 mL)
2. washthe organic phase was washed with brine
3. dry with materialdried (Na2SO4)
4. filtrationfiltered
5. customevaporated
6. customto give an oily residue (NMP residues)
7. customThe crude material was further purified by HPLC

ORDレコード

ord-3bcbb55fb6c24facb6eab3f2def3d61d

出典データセット

uspto-grants-2011_10

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08030340B2