- Synthesis of N,N-dialkyl-9-oxoacridine-10(9H)-carbothioamides via the reaction of (2-halophenyl)(2-isothiocyanatophenyl)methanones with secondary amines, followed by cyclization with NaH
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The first preparation of acridin-9(10H)-ones carrying a tertiary thiocarbamoyl group at C(10), i.e., N,N-dialkyl-9-oxoacridine-10(9H)- carbothioamides 9, is described. The method is based on the reaction of (2-halophenyl)(2-isothiocyanatophenyl)methanones 7, prepared from (2-aminophenyl)(2-halophenyl)methanones 5 by a convenient three-step sequence, with secondary amines in DMF at room temperature to generate the corresponding thiourea derivatives 8 in situ, which are treated with NaH at 100-120° to provide the desired products in one-pot reactions in generally good yields.
- Kobayashi, Kazuhiro,Nakagawa, Kazuhiro,Yuba, Shohei
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p. 2033 - 2039
(2013/12/04)
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- SUBSTITUTED-1,4-DIAZEPINES
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The invention relates to new 1,4-diazepines of the general formula STR1 in which R 1, R 2 R 3, X and A have the meaning indicated in the specification.The new compounds are intended for use for the treatment of pathological states and diseases in which PAF (platelet activating factor) is involved.
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