Extracurricular laboratory: Synthetic route of 6228-73-5

The synthetic route of 6228-73-5 has been constantly updated, and we look forward to future research findings.

6228-73-5, name is Cyclopropanecarboxamide, belongs to amides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Application In Synthesis of Cyclopropanecarboxamide

The product from step 1 (30 mg, 0.080 mmol), cyclopropanecarboxamide (13.59 mg, 0.160 mmol), Xantphos (9.24 mg, 0.016 mmol)And cesium carbonate (78 mg, 0.239 mmol)The mixture in dioxane (0.8 mL) was purged for 5 min,Then Pd2 (dba) 3 (7.31 mg, 7.98 mumol)And the reaction was placed in a preheated chamber at 130 C for 1 h. The reaction mixture was then cooled and diluted with DMSO and purified by reverse phase preparative LCMS using the following conditions: Column: Waters XBridge C18, 19 x 200 mm, 5 mum particles; mobile phase A: 5: 95 acetonitrile: water MM ammonium acetate); mobile phase B: 95: 5 acetonitrile: water (with 10 mM ammonium acetate); gradient: 0-100% B over 20 minutes and then at 100% B for 0 min; flow rate: 20 mL / min The The fractions containing the desired product are combined and dried by centrifugal evaporation. The yield of the product was 26.3 mg (69%).

The synthetic route of 6228-73-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; MOSLIN,, RYAN M.; WEINSTEIN,, DAVID S.; WROBLESKI,, STEPHEN T.; ZHANG,, YANLEI; TOKARSKI,, JOHN S.; MERTZMAN,, MICHAEL E.; LIU,, CHUNJIAN; (124 pag.)TWI582077; (2017); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics