- WO2010036831 Preparation of a quinolinyloxydiphenylcyclopropanedicarboxamide

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Biological target:

hepatocyte growth factor receptor or c-Met

Activity:

Inhibitor

Steps Conditions Reactions
a Et3N / SOCl2 / THF Amide synthesis (Coupling reaction)
b oxalyl chloride / THF Amide synthesis (Coupling reaction)
Steps Conditions Reactions
a K2CO3 / tetrabutylammonium bromide Ether synthesis (Nucleophilic substitution)
b H2SO4 / HNO3 Nitration
c Morpholine / K2CO3 / KI / tetrabutylammonium bromide / H2O Tertiary amine synthesis (nucleophilic substitution)
d Formic acid  /potassium formate / Pd-C / EtOH / H2O Primary amine synthesis (Nitro reduction)
e EtONa / ethyl formate / EtOH Cyclisation
f POCl3 / ACN Chlorination
Steps Conditions Reactions
a

1. LiOH / 1,3,2-dioxathiane-2,2-dioxide / THF

2. Morpholine / THF 


Steps Conditions Reactions
a Pd(AcO)2 / racemic-2-(di-tert-butylphosphino)-1,1'-binaphthyl / K3PO4 / Toluene Buchwald-Hartwig reaction

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