VERFAHREN ZUR HERSTELLUNG VON NEUEN CHINAZOLINVERBINDUNGEN UND DEREN SAUREADDITIONSSALZEN UND OPTISCH AKTIVEN FORMEN

Procedure for preparing quinazoline derivatives, of formula: **(See formula)** wherein (i) R1 is a hydrogen atom or a lower alkyl group; (R2) n represents 1 to 3 optional substituents, each R being a hydrogen atom or a lower hydroxy or alkoxy group and a being 1 to 3, or any two of the B2 moieties c...

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Hauptverfasser: THOMSON COLIN DR, DANILEWICZ JOHN CHRISTOPHER DR, HAM ALLAN LESLIE, EVANS ANTHONY GARTH
Format: Patent
Sprache:ger
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Zusammenfassung:Procedure for preparing quinazoline derivatives, of formula: **(See formula)** wherein (i) R1 is a hydrogen atom or a lower alkyl group; (R2) n represents 1 to 3 optional substituents, each R being a hydrogen atom or a lower hydroxy or alkoxy group and a being 1 to 3, or any two of the B2 moieties constituting a methylenedioxy or ethylenedioxy group attached to positions adjacent to ring A; (ii) X represents -CH2) p where p is 1 to 3, -CH = CH- or -0CH2 CH = CH (iii) Y is attached to position 3 or 4 of ring C and represents: (a) a group of formula -Z1-COR3, where Z1 is -CH2-or (see formula), R3 is a lower alkyl group optionally substituted by an amino, hydroxy, lower alkoxy, aryl or heteroaryl group; a lower alkenyl- or lower alkynyl-methyl group; a lower alkoxy group optionally substituted by an amino, aryl, heteroaryl, lower alkoxy or hydroxy group; an aryl group; an aryloxy group; or a heteroaryl group; and R4 is a hydrogen atom; a lower alkyl group optionally substituted by an amino, lower alkoxy, hydroxy, carbotoxy, aryl or heteroaryl group; a lower alkenyl- or lower alkynyl-methyl group; an aryl group or a heteroaryl group; (b) a group of the formula: **(See formula)** wherein R5 is a group or as defined above for R3 or is a group of formula: **(See formula)** wherein R7 is a hydrogen atom or a lower alkyl group and R6 is a group as defined above for R4, or R6 and R7 taken together with the nitrogen atom to which they are attached form a saturated monocyclic heterocyclic ring; or (c) a group of the formula: **(See formula)** wherein Z2 is Z1 or -O- and R6 and R7 are defined or as above, provided that when Z2 is (see formula), R4 and R7 taken together may represent - (CH2) 2-, - (CH2) 3 - or an o-phenylene group; and (iv) R is a hydrogen atom or a lower alkyl group attached to the same carbon atom as Y; provided that when Z is -CH = CH- or -CHsCH = GH-, R is absent and Y is -CH2COR3, -CH2CON (R6) (R7) or -CH2CSN (R6) (R7) where R3, R6 and R7 are defined or as above, Y being attached to an unsaturated ring carbon atom; characterized in that it comprises reacting a quinazoline of the formula: **(See formula)** where R1, R2 and n are defined as above and Q1 is a good leaving group, such as chlorine or bromine, with an amine of formula: **(See formula)** wherein X, Y and E are defined as above, any R2 and Y groups being protected or capable of displacing the leaving group Q1, prior to the reaction and deprotected after the reaction; and then recovering th