发明名称 PROCESS FOR PREPARING LEUKOTRIENE ANTAGONISTS
摘要 Benzene derivs. I [R1=R5-CO-, halo; R2=OH, halo; R3=C1-12 alkyl, substituted C1-12 alkyl, C2-6 alkenyl; Y=0, S(O)p, CR6R7; Z=0, S(O)p, CR8R9; R5=H, C1-6 alkyl, C3-8 cycloalkyl, halo, C1-4 alkyl, C1-4 alkoxy; R6, R7=H, C1-10 alkyl, Ph, Benzyl; R8, R9=H, C1-10 alkyl, Ph, Benzyl; n=1-10; p=0,1, or 2; D=CN, SCN, etc.! were prepd. Thus, 10.2 g 4-(2-propyl-3,4-dichloro-phenyxy)pentane nitrile in 80 ml dimethyl formamide was treated with 23.27 g sodium azide and 18.97 g NH4Cl. This mixt. was mixed for 2 days under a N-pressure at 120≦̸C and cooled to room temp. to give 47.9g 5-[4-(2-propyl-3,4- dichlorophenoxy)butyl-tetrazole[A!. At 1x10-6M, the compd. [A! gave 94% inhibition of leukotriene D4-induced contractions of guinia pig ileum in vitro.
申请公布号 KR860001980(B1) 申请公布日期 1986.11.07
申请号 KR19840004213 申请日期 1984.07.18
申请人 ELI LILLY & CO. 发明人 HERRON, DAVID KENT
分类号 C07C33/46;A61K31/045;A61K31/12;A61K31/135;A61K31/155;A61K31/16;A61K31/19;A61K31/215;A61K31/26;A61K31/275;A61K31/41;A61P11/00;A61P37/08;A61P43/00;C07C39/27;C07C39/367;C07C43/178;C07C43/225;C07C43/23;C07C47/56;C07C47/575;C07C49/82;C07C49/84;C07C57/30;C07C57/58;C07C59/52;C07C59/56;C07C59/64;C07C59/66;C07C59/68;C07C59/74;C07C59/88;C07C59/90;C07C69/65;C07C69/708;C07C69/73;C07C255/32;C07D257/04;C07D257/06;C07D295/088;(IPC1-7):C07D257/04 主分类号 C07C33/46
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