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1.本文叙述三系列共十九种与放线菌素有关的类似物——吩噁嗪酮-(3)衍生物的合成。 2.2-硝基3-甲氧基-4-取代基-苯甲酸(Ⅳa—c,R=OCH_3、OC_2H_5及CH_3)与强碱水溶液共热时,可选择水解邻位于硝基的醚键,生成相应的邻硝基酚衍生物(Va—c)。 3.作者等提出一将邻-氨基酚类化合物(Ⅻa、Ⅻc、Ⅻd及Ⅻi)氧化成2-氨基-吩噁酮-(3)衍生物(ⅩⅫa、ⅩⅫc、ⅩⅫd及ⅩⅫi)的新方法,即在中性乙醇溶液中以钯-炭或Raney镍为催化剂,用空气氧进行氧化。此法操作简便,产量尚佳,克服某些邻-氯基酚类化合物在磷酸缓冲液或碳酸铵稀醇溶液中溶解度小的困难。 4.初步药理实验结果表明,肉瘤180(固体型)对某些所合成的化合物敏感。结果将在他处发表。
1. This article describes the three series of 19 kinds of actinomycin-related analogues - phenoxazinone - (3) derivatives. 2.2-Nitro-3-methoxy-4-substituent-benzoic acid (Ⅳa-c, R = OCH 3, OC 2 H 5 and CH 3) can co-hydrolyze the ether bond adjacent to the nitro group The corresponding o-nitrophenol derivatives (Va-c). 3. The authors propose a new method for the oxidation of o-aminophenols (Ⅻa, Ⅻc, Ⅻd and Ⅻi) to 2-amino-phenoxanone- (3) derivatives (XXIIa, XXIIc, XXII and XXII) That is, in a neutral ethanol solution with palladium - carbon or Raney nickel as a catalyst, the oxidation with air oxygen. This method is simple and easy to operate with good yield and overcomes the difficulty of some o-chlorophenols dissolving little in phosphate buffer or ammonium carbonate dilute alcohol solution. 4. Preliminary pharmacological experiments show that sarcoma 180 (solid type) is sensitive to some of the compounds synthesized. The results will be published elsewhere.