发明名称 СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ МОРФОЛИНА И ИХ ПРОМЕЖУТОЧНЫХ СОЕДИНЕНИЙ
摘要 Processes for the preparation of a compound of formula (IIIA)(I), or a salt thereof; wherein; Z represents a bond, CO, SO2, CR<10>R<7>(CH2)n, (CH2)nCR<10>R<7>, CHR<7>(CH2)n<O>, CHR<7>(CH2)nS, CHR<7>(CH2)nOCO, CHR<7>(CH2)nCO, COCHR<7>(CH2)n or SO2CHR<7>(CH2)n; R<6> represents C1-6 alkyl, C2-6 alkenyl, aryl, heteroaryl, aryl-C2-6 alkenyl-, -CN or a group of formula -Y<2>-J<3>; R<7> represents hydrogen, C1-4 alkyl, CONR<8>R<9> 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<3> represents a moiety of formula (K): (II), wherein X<1> represents oxygen, NR<11> or sulphur, X<2> represents CH2, oxygen, NR<12> or sulphur, m<1> represents an integer from 1 to 3 and m<2> represents an integer from 1 to 3, provided that m<1>+m<2> is in the range from 3 to 5, also provided that when both X<1> and X<2> represent oxygen, NR<11>, NR<12> or sulphur, m<1> and m<2> must both not equal less than 2, wherein (K) is optionally substituted by one or more (eg. 1 or 2) -Y<3>-aryl, -Y<3>-heteroaryl, -Y<3>-CO-aryl, -COC3-8 cycloalkyl, -Y<3>-CO-heteroaryl, -C1-6 alkyl, -Y<3>-COOC1-6 alkyl, -Y<3>-COC1-6 alkyl, -Y<3>-W, -Y<3>-CO-W, -Y<3>-NR<15>R<16>, -Y<3>-CONR<15>R<16>, hydroxy, oxo, -Y<3>-SO2NR<15>R<16>, -Y<3>-SO2C1-6 alkyl, -Y<3>-SO2aryl, -Y<3>-SO2heteroaryl, -Y<3>-NR<13>C1-6 alkyl, -Y<3>-NR<13>SO2C1-6 alkyl, -Y<3>-NR<13>CONR<15>R<16>, -Y<3>-NR<13>COOR<14> or -Y<3>-OCONR<15>R<16> groups, and is optionally fused to a monocyclic aryl or heteroaryl ring; R<8>, R<9>, R<10>, R<11>, R<12>, R<13> and R<14> independently represent hydrogen or C1-6 alkyl; R<15> and R<16> independently represent hydrogen or C1-6 alkyl or R<15> and R<16> together with the nitrogen atom to which they are attached may form a morpholine, piperidine or pyrrolidine ring; R<17> and R<18> 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<1>, Y<2> and Y<3> independently represent a bond or a group of formula -(CH2
申请公布号 RU2004125289(A) 申请公布日期 2005.06.27
申请号 RU20040125289 申请日期 2003.03.27
申请人 Глаксо Груп Лимитед (GB) 发明人 ХЕЙЗ Мартин Алистер (GB);МИЛЛЗ Гейл (GB);СУОНСОН Стивен (GB);УОКЕР Эндрю Джон (GB);УИЛКИНСОН Марк (GB)
分类号 C12P17/14;C07C213/04;C07C215/12;C07D209/48;C07D265/30;C07D413/04;C07D413/06 主分类号 C12P17/14
代理机构 代理人
主权项
地址