Diisopropylethylamine → HCID 66613368、化合物

2-(7-Aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HATU) (1.9 g, 5 mmol) and diisopropyl ethyl amine (DIEA) (2.7 mL) was added to a suspension of 4-(tert-butoxycarbonyl)thiomorpholine-2-carboxylic acid (1.3 g, 5 mmol) in DMF (10 mL) and was stirred at room temperature for 15 minutes. Methyl 5-amino-1H-indazole-3-carboxylate (0.95 g, 5 mmol)) was added to the reaction and was stirred at room temperature for an additional 30 minutes. The reaction was quenched with water (50 mL) and extracted with ethyl acetate (3×20 mL). The extracts were combined, dried using anhydrous sodium sulfate, filtered, and concentrated in vacuo. The crude product (2.1 g) was progressed to the next step without purification.

1. stirringwas stirred at room temperature for an additional 30 minutes
2. customThe reaction was quenched with water (50 mL)
3. extractionextracted with ethyl acetate (3×20 mL)
4. customdried
5. filtrationfiltered
6. concentrationconcentrated in vacuo
7. customThe crude product (2.1 g) was progressed to the next step without purification

ORDレコード

ord-050bb8362c594cab9053cd6c1e049907

出典データセット

uspto-grants-2015_02

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08946216B2