共查询到19条相似文献,搜索用时 218 毫秒
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3-甲基吡啶-2-甲酸甲酯(2)经氧化、硝化和还原反应制得4-氨基-3-甲基吡啶-2-甲酸甲酯(5),然后经改进的Balz-Schiemann反应制得4-氟-3-甲基吡啶-2-甲酸甲酯(1),以2计总收率约18%。 相似文献
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5-乙基-2-甲基吡啶经选择性氧化、酯化、LiAlH4还原和PCC氧化等反应得到6-甲基吡啶-3-甲醛,总收率47%. 相似文献
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报道了3-氨甲基吡啶的合成工艺改进,在常温、常压条件下,采用催化氢化的方法合成了3-氨甲基吡啶。该法易于工业化生产。 相似文献
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目的 获得2-甲基-3-羟基吡啶合成方法,降低2-甲基-3-羟基吡啶的合成成本,为常山酮等药物的合成提供了廉价原料。方法 分别以天冬氨酸和丙氨酸为起始原料,经过噁唑中间体,利用Diels-Alder反应,最后脱羧获得2-甲基-3-羟基吡啶,总收率7.4%和30.3%。结果 提供了1种合成2-甲基-3-羟基吡啶的方法,丙氨酸为原料的方法更适合工业化生产,且合成方法简单、原料价格低廉,极大降低了2-甲基-3-羟基吡啶的合成成本,为常山酮等药物的合成提供了廉价原料。 相似文献
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2-氨基-3-甲基吡啶(1)是制备多种药物的中间体。文献以2-氰基-3-甲基吡啶为原料、过氧化氢为氧化剂,碱性条件下不完全水解氰基得3-甲基-2-吡啶甲酰胺,再经Hoffman降解得1,总收率74%,此法原料较贵,中间体均须分离纯化,操 相似文献
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1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸单甲酯(1)是二氢吡啶类降压药的重要中间体。主要合成方法如下:(1)1,4.二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸甲基氰乙基酯经碱性水解制得,收率60%,但原料不易得;(2)1-乙氧甲基-1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶羧酸二甲酯在金属钠和二甲胺基异丙醇存在下水解、酸化制得,收率47.4%,操作繁琐,后处理困难; 相似文献
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E. S. Nikitskaya E. I. Levkoeva V. S. Usovskaya M. V. Rubtsov 《Pharmaceutical Chemistry Journal》1967,1(3):160-163
Some new alkamino esters of quinuclidine-2-carboxylic, 1,6-dimethylpiperidine-2-carboxylic and 6-methylpyridine-2-carboxylic acid and their quaternary salts have been synthesized for pharmacological study. The methods of synthesis for some alkamino alcohols are described.Translated from Khimiko-Farmatsevticheskii Zhurnal, No. 3, pp. 48–51, March, 1967. 相似文献
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H Yamada H Tobiki K Jimpo T Komatsu T Okuda H Noguchi T Nakagome 《The Journal of antibiotics》1983,36(5):543-551
The influence of various 3-substituents on the antibacterial activity of 7 beta-[D-2-(4-hydroxy-6-methylpyridine-3-carbonylamino)-2-(4-hydroxyphenyl) acetamido]ceph-3-em-4-carboxylic acids (III) was investigated. Introduction of an acidic substituent, such as a sulfo or a carboxyl group, to a 3-(1-methyl-1H-tetrazolyl)thiomethyl substituent (IIIf--i) resulted in a marked loss of activity against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus faecalis, Escherichia coli, Klebsiella pneumoniae, and Enterobacter aerogenes, in contrast to an in crease of activity against Proteus mirabilis. Displacement of the acetoxy group of IIIb with pyridines (IIIm--p) enhanced the activity against P. aeruginosa and E. aerogenes: their activity against those strains were superior to that of the cephalosporin IIId having a 3-(1-methyl-1H-tetrazolyl)thiomethyl substituent. As a result of extensive studies in addition to the study of in vitro activity in this series, 7 beta-[D-2-(4-hydroxy-6-methylpyridine-3-carbonylamino)-2-(4-hydroxyphenyl) acetamido]-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxylic acid, code No. SM-1652, cefpiramide (generic name), was selected as a candidate for further biological and clinical investigations. 相似文献
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3-取代-5-氟-1-2-二氢-3H-吲哚-2-酮类化合物的合成及抗肿瘤活性 总被引:1,自引:0,他引:1
5-溴-1H-吲哚经氰基取代、Vilsmeier-Haack反应、水解、缩合制得3-[(Z)-(5-氟-1,2-二氢-2-氧代-3H-亚吲哚基)甲基]-1H-吲哚-5-甲酸,再和相应的胺类化合物反应制得10个3-取代-5-氟-1,2-二氢-3H-吲哚-2-酮类化合物.以舒尼替尼为阳性对照,用MTT法测试目标化合物对人乳腺上皮细胞HMEC的体外抑制活性,其中1c、1f、1g和1h在浓度为10 μmol/L时,对HMEC的抑制活性优丁舒尼替尼.进一步测试1c和1e对SGC7901、A549、HL-60、SK-BR-3、HCT116肿瘤细胞株的抗增殖活性.结果表明,1c和1e对白血病细胞株HL-60的抗增殖活性优丁舒尼替尼. 相似文献
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目的制备5-甲氧基-1H-吡咯并[3,2-b]吡啶-2-甲酸。方法以2-甲基-6-氯-3-硝基吡啶为原料,经Williamson合成法制得2-甲基-6-甲氧基-3-硝基吡啶,再经Reissert合成法制得终产物。结果反应总收率33%,产物结构由1H-NMR光谱确证。结论该方法简单、原料价廉易得,后处理容易,副产物较少,适于工业化生产。 相似文献
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2,6-Dimethyl-4-(3′-nitrophenyl)-3-methoxylaminocarbonyl-1,4-dihydropyridine-5-carboxylic acid methylester,3b reacted with 2-cyanoethanol or benzylalcohol to give the corresponding cyanoethylurethane compound6c in 40.6% yield and benzylurethane compound6d in 32% yield. The cyanoethylurethane6c was hydrolized in ethanolic NaOH to give 2,6-dimethyl-4-(3′-nitrophenyl)-1,4-dihydropyridine-3-amino-5-carboxylic acid 5-methyl
ester. HCl8 in 64.8% yield. Another acid hydrolysis of benzylurethane6d gave 2,6-dimethyl-4-(3′-nitrophenyl)-1,4-dihydropyridine-3-amino-5-carboxylic acid 5-methylester. HBr11 in 54.7% yield. 相似文献