FIELD: chemistry.
SUBSTANCE: present document discloses a method for synthesis of quinazoline compounds of formula (I)
involving: (a) contacting a compound of formula (II)
with an organomagnesium compound and a zinc complex at a temperature of −80 °C to about −60 °C in a polar aprotic solvent, (b) bringing the mixture from step (a) into contact with (i) a compound of formula (III)
(ii) a Pd or Ni-based catalyst precursor and (iii) a chiral ligand of formula (L1)
at temperature of 30 °C to about 65 °C for 10 to about 30 hours, thus synthesis of the compound of formula (I).
EFFECT: improved methods are developed for atroposelective synthesis of aminopyridinyl-quinazolinyl compounds by means of Negichi coupling using a chiral ligand.
49 cl, 7 tbl, 25 ex, 6 dwg
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