PROCESS FOR THE PREPARATION OF MORPHOLINE DERIVATIVES AND INTERMEDIATES THEREFORE

Processes for the preparation of a compound of formula (IIIA)(I), or a salt thereof; wherein; Z represents a bond, CO, SO2, CR R (CH2)n, (CH2)nCR R , CHR (CH2)n, CHR (CH2)nS, CHR (CH2)nOCO, CHR (CH2)nCO, COCHR (CH2)n or SO2CHR (CH2)n; R represents C1-6 alkyl, C2-6 alkenyl, aryl, heteroaryl, aryl-C2-...

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Hauptverfasser: HAYES, MARTIN ALISTAIR, SWANSON, STEPHEN, WILKINSON, MARK, WALKER, ANDREW JOHN, MILLS, GAIL
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:Processes for the preparation of a compound of formula (IIIA)(I), or a salt thereof; wherein; Z represents a bond, CO, SO2, CR R (CH2)n, (CH2)nCR R , CHR (CH2)n, CHR (CH2)nS, CHR (CH2)nOCO, CHR (CH2)nCO, COCHR (CH2)n or SO2CHR (CH2)n; R represents C1-6 alkyl, C2-6 alkenyl, aryl, heteroaryl, aryl-C2-6 alkenyl-, -CN or a group of formula -Y -J ; R represents hydrogen, C1-4 alkyl, CONR R or COOC1-6 alkyl;a and b represent 1 or 2, such that a+b represents 2 or 3;n represents an integer from 0 to 4; M represents a C3-8 cycloalkyl or C3-8 cycloalkenyl group fused to a monocyclic aryl or monocyclic heteroaryl group; J represents a moiety of formula (K): (II), wherein X represents oxygen, NR or sulphur, X represents CH2, oxygen, NR or sulphur, m represents an integer from 1 to 3 and m represents an integer from 1 to 3, provided that m +m is in the range from 3 to 5, also provided that when both X and X represent oxygen, NR , NR or sulphur, m and m must both not equal less than 2, wherein (K) is optionally substituted by one or more (eg. 1 or 2) -Y -aryl, -Y -heteroaryl, -Y -CO-aryl, -COC3-8 cycloalkyl, -Y -CO-heteroaryl, -C1-6 alkyl, -Y -COOC1-6 alkyl, -Y -COC1-6 alkyl, -Y -W, -Y -CO-W, -Y -NR R , -Y -CONR R , hydroxy, oxo, -Y -SO2NR R , -Y -SO2C1-6 alkyl, -Y -SO2aryl, -Y -SO2heteroaryl, -Y -NR C1-6 alkyl, -Y -NR SO2C1-6 alkyl, -Y -NR CONR R , -Y -NR COOR or -Y -OCONR R groups, and is optionally fused to a monocyclic aryl or heteroaryl ring; R , R , R , R , R , R and R independently represent hydrogen or C1-6 alkyl; R and R independently represent hydrogen or C1-6 alkyl or R and R together with the nitrogen atom to which they are attached may form a morpholine, piperidine or pyrrolidine ring; R and R independently represent hydrogen or C1-6 alkyl; W represents a saturated or unsaturated, non-aromatic 5-7 membered ring containing between 1 and 3 heteroatoms selected from nitrogen, oxygen or sulphur, optionally substituted with one or more C1-6 alkyl, halogen or hydroxy groups; Y , Y and Y independently represent a bond or a group of formula -(CH2