Development of a new practical synthesis of a 5-HT2C receptor agonist
A new practical synthesis of a 5-HT2C receptor agonist has been developed and implemented on multikilogram scale. The key step, the selective epoxide opening in the glycidyl tosylate with the aryl Grignard reagent, allowed the incorporation of this commercially available chiral C3 synthon into the molecule and elaboration of the resulting intermediate into the target aminomethyldihydrobenzofuran without loss of enantiomeric purity.
ASYMMETRIC SYNTHESIS OF SUBSTITUTED DIHYDROBENZOFURANS
The present invention concerns production of a compound of the formula (I) or a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula (II) where Ar, Y, R1, RY, R2, and m are as defined herein.
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(2010/11/08)
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