A search for suitable reaction conditions for the preparation of 4-phenyldihydropyrimidinone derivative 6, activated by CeCl 3 and InCl 3 [equimolar or catalytic amount (20%)] revealed that the reaction proceeds in good yields (65-92% yield) in THF or toluene as a solvent. The preparation of enantiomerically enriched compound 6 was achieved in moderate enantioselectivity (8-40% ee) by a modified one-pot Biginelli condensation procedure in the presence of the chiral ligands (R,R)-13 or (S,S)-14.
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Muñoz‐Muñiz et al. (2003) studied this question.