Process for preparing heterocyclic derivatives

Details Process for preparing heterocyclic derivatives Process for preparing heterocyclic derivatives

2009-10-29

2010-11-23

Saeed, Kamal A (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C548S263200

Reexamination Certificate

active

07838680

ABSTRACT:
The present invention relates to a novel process, useful for preparing key intermediates of formula (I) in the synthesis of various compounds, among them compounds which are potent and specific antagonists of D3 receptors,in whichX may be Nitrogen or Sulfur;Het means aryl or heteroaryl; each of which may be substituted by 1 to 4 groups J selected from:halogen, C1-C6 alkyl C1-C6 alkoxy, halo C1-C6 alkyl C2-C6 alkenyl,C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R1, nitro, hydroxy, —NR2R3, cyano or a group Z;R1is a C1-C4 alkyl —OR3or —NR3R4;R2is hydrogen or C1-C6 alkyl;R3is hydrogen or C1-C6 alkyl;R is H, C1-C6 alkyl aryl, benzyl; each of which may be substituted by 1 to 4 groups J;according to the following Scheme 1:in whichstep a means a reaction in basic conditions of compounds (IIA) with 3-thiosemicarbazide derivatives, followed by a treatment with an inorganic base and n-propane phosphonic cyclic anhydride and final pH adjustment with inorganic acids to give compounds of formula (II).

REFERENCES:
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