BCX-1170

Chemical Name: Furan-2-carboxylic acid 4-[3-amino-3-imino-1(E)-propenyl]phenyl ester methanesulfonate
项目整合开发状态: Preclinical
项目研究机构: BioCryst (Originator)
合成路线:The reaction of 4-hydroxybenzaldehyde (I) with cyanacetic acid (II) by means of pyridine in toluene gives the 3-(4-hydroxyphenyl)propenenitrile (III),which by reaction first with methanolic HCl and then with methanolic ammonia is converted into the amidine (IV).Finally,this compound is condensed with 2-furylcarbonyl chloride (V) in pyridine and treated with methanesulfonic acid to afford the target sulfonate.

合成路线:The acylation of (E)-3-(4-hydroxyphenyl)-2-propenamide (VI) with acetic anhydride gives the 4[(E)-3-amino-3-oxo-1-propenyl]phenyl acetate (VII),which by reaction first with BF3 ethearate and then with ammonia is converted into the amidine (IV).Finally,this compound is condensed with 2-furylcarbonyl chloride (V) in pyridine and treated with methanesulfonic acid to afford the target sulfonate.