发明名称 SYNTHESIS OF GLYT-1 INHIBITORS
摘要 Process for preparation of a compound of formula (I) wherein Het is a 6-m embered heteroaryl group, containing one, two or three nitrogen atoms; R1 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl, NR4R5 or (C1-C6)-alkyl subtituted by hal ogen; R2 is hydroxy, halogen, NO2, CN, (C1-C6)-alkyl, (C3-C6)-cycloalkyl, (C 1-C6)-alkyl substituted by halogen, (C1-C6)-alkyl substituted by hydroxy, (C H2)o-(C1-C6)-alkoxy, (C1-C6)-alkoxy substituted by halogen, NR4R5, C(O)R6 or SO2 R7; R3 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl or (C1-C6)-alkyl subtituted by halogen; R4 and R5 independently from each other are hydrogen or (C1-C6) -alkyl; R6 is hydrogen, (C1-C6)-alkyl, (C1-C6)-alkoxy or NR4R5; R7 is (C1-C6 )-alkyl, (C1-C6)-alkyl optionally subtituted by halogen, (CH2)o-(C3-C6)-cycl oalkyl, (CH2)o-(C3-C6)-alkoxy or NR4R5; n is 0, 1, 2 or 3; o is 0, 1 or 2; a nd pharmaceutically acceptable acid addition salts thereof, characterized in that it comprises the steps of a) reacting a compound of formula (21) with a compound of formula: R3 OH 8 to a compound of formula (11) and b) coupling the compound of formula (11) in the presence of a coupling reagent or the c orresponding acid halogenide with a compound of formula (15) to obtain a com pound of formula (I).
申请公布号 CA2678630(A1) 申请公布日期 2008.09.12
申请号 CA20082678630 申请日期 2008.02.25
申请人 F. HOFFMANN-LA ROCHE AG 发明人 WALDMEIER, PIUS;WANG, SHAONING;PFLEGER, CHRISTOPHE
分类号 A61K31/497;A61P25/00;C07D213/74 主分类号 A61K31/497
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