乙酰甲基

Methods Starting from 2-chloro-4-nitrophenol and 2- pyridine hydrochlorid, 3-chloro-4-(pyridin-2-ylmethoxy) aniline was obtained via etherization and reduction. The obtained aniline coupled with N-(4-chloro-3-cyano-7-ethoxyquinolin-6-yl) acetamide to give 4-[3-chloro-4-(2-pyridylmethoxy) phenylamino]-3-cyano-7-ethoxy-6-N-acetylaminoquinoline. And then it was deacetylated, followed by reacting with4- but-2-enoyl chloride to yield the target compound neratinib.

以2-氯－4-硝基苯酚和2-氯甲基吡啶为起始原料，经醚化、硝基还原得到3-氯－4-（吡啶－2-甲氧基）苯胺，3-氯－4-（吡啶－2-甲氧基）苯胺与3-氰基－6-乙酰氨基－7-乙氧基－4-氯喹啉反应得到3-氰基－6-乙酰氨基－4-［3-氯－4-（吡啶－2-甲氧基）苯氨基］－7-乙氧基喹啉，3-氰基－6-乙酰氨基－4-［3-氯－4-（吡啶－2-甲氧基）苯氨基］－7-乙氧基喹啉去乙酰保护基后，与-4-二甲氨基－2-丁烯酰氯经酰化反应得到ner-atinib。

When the catalyst was triethylamine, the water produced in condensation of isopropanolamine or ethanolamine and butanone was removed with benzene by water segregator, then the dichloroacetyl chloride was dropped.

利用异丙醇胺、乙醇胺、丁酮和二氯乙酰氯为原料，分别合成了两种除草剂安全剂Ⅰ∶3-二氯乙酰基-2，5-二甲基-2-乙基-1，3-噁唑烷和Ⅱ∶3-二氯乙酰基-2-甲基-2-乙基-1，3-噁唑烷。

Formyl-3-acetyl-4-methyl-5-carbobenzoxypyrrole (6) was synthesized via the selective oxidation of 2,4-dimethyl-3-acetyl-5-carbobenzoxypyrrole (5), which was produced from acetylacetic benzylester (1) via nitrosation, reduction and addition-cyclization with acetylacetone. The total yield of the product was about 34%.

以乙酰乙酸苄酯(1)为原料，经过亚硝化、还原、与乙酰丙酮加成环化生成2， 4-二甲基－3-乙酰基－5-苄氧羰基吡咯(5)，通过选择性氧化反应制得目标化合物2-甲酰基－3-乙酰基－4-甲基－5-苄氧羰基吡咯(6)，反应的总收率约为34%。

Synthesis process of 2,6-dichloro-3-methylaniline was investigated 3-methylaniline was first N-acetylated with acetic anhydride,then treated with chlorosulphonic acid and ammonia yielding the 2-methyl-4--benzenesulfonic amide,which wasin turn deacetylated,chlorinated and hydrolyzed to the title compound.Hydrochloric acid was used instead of sodium hydroxide in deacetylation and sodium chlorate instead of hydrogen peroxide as oxidant in chlorination.

合成工艺2，6-二氯-3-甲基苯胺调查3-甲基首次N-乙酰与醋酸酐，然后与氯磺酸和氨产量 2-甲基-4--苯磺酰胺基，而擅转乙酰，氯化和水解的标题compound.hydrochloric酸代替氢氧化钠乙酰氯酸钠代替双氧水为氧化剂，加氯。

Synthesis of Antidote of N-Dichloroacetyl-2-methyl-1-oxa-4-aza-spiro-4.4-nonane BI Hong-mei, ZHANG Jin-yan, LIANG Ying, SHEN Yong (College of Arts and Sciences Heilongjiang August First Reclamation University, Daqing 163319, Heilongjiang, China) Abstract: N-Dichloroacetyl-2-methyl-1-oxa-4-aza-spiro-4.4-nonane was synthesized by one pot method with isopropanolamine, cyclopentanone and dichloroacetyl chloride. The optimum reaction conditions obtained are as follows:the proportion in moles of the above materials is 1∶1∶1.2, reaction solvent is toluene, reaction temperature is -15 to -10 ℃,reaction time is 3 h, under the optimum condition, the yield of the compound is 50.0%.

除草剂解毒剂N-二氯乙酰基-2-甲基-1-氧杂-4-氮杂-螺[4.4]壬烷的合成毕洪梅，张金艳，梁英，沈勇(黑龙江八一农垦大学文理学院，黑龙江大庆 163319)摘要：以33%的氢氧化钠水溶液为缚酸剂，异丙醇胺、环戊酮和二氯乙酰氯为原料，采用&一锅法&合成了N-二氯乙酰基-2-甲基-1-氧杂-4-氮杂-螺[4.4]壬烷，采用正交实验法得到最佳反应条件：反应原料摩尔比为1∶1∶1.2，苯作溶剂，反应的温度为-15 ℃~-10 ℃，搅拌时间为3 h，产率达到50.0%。

Then sodium ethoxide was used as base,the nucleophilic substitution of 2-pyrrolidone with the intermediate provided nefiracetam.

以碳酸钠为缚酸剂，摩尔比为1︰1的2，6-二甲基苯胺与氯乙酰氯反应合成了中间体2-氯-N-(2，6-二甲基苯基)乙酰胺；在强碱乙醇钠作用下，2-吡咯烷酮再与2-氯-N-(2，6-二甲基苯基)乙酰胺经亲核取代合成了目标化合物奈非西坦。

The famciclovir was synthesized from purine by a series of steps by Acylation, Decarboxylation, Reduction ,and so on; Derivatives of these intermediates is described from the 6-chloro- 9H- purin-2-amine as raw materials in different conditions when the iodine and bromide were synthesized with the addition of two intermediate 6-bromo-9H-purin-2-amine and 6-iodo-9H-purin-2-amine; There is elaborated from the main part of a acetophenone, urineaminohydrochloride, phenylhydrazine, ethyl acetoacetate as raw material through a series of reactions to synthetic 3-phenyl-4-formylphenyl pyrazole and 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-aldehyde two pyrazole aldehyde, and then with 2-amino-6-chlorine-9-(2-methicillin-oxo-co-methyl-4-yl) purine reaction of the two new pyrazole purine Schiff bases.

本论文主是采用以鸟嘌呤为原料，经过一系列的酰基化，脱羧，还原等反应作用下最终得到了产物2-氨基-9-(4-乙酰氧基-3-乙酰氧基甲基丁基)嘌呤；其中的中间体衍生物主要是阐述从以2-氨基-6-氯鸟嘌呤为原料通过在不同的条件下进行溴代与碘代分别合成了另外两种中间体2-氨基-6-溴鸟嘌呤及2-氨基-6-碘鸟嘌呤；还有一部分主要是阐述从以苯乙酮，盐酸氨基脲，苯肼，乙酰乙酸乙酯为原料通过一系列的反应先合成3-苯基-4-醛基吡唑及5-氯-3-甲基-1-苯基-1H-吡唑-4-甲醛这两个吡唑醛，然后再与2-氨基-6-氯-9-(2-甲氧羰基丁酸甲酯-4-基)嘌呤反应得到了两个新型的吡唑嘌呤席夫碱

In the first part, five new 4-acyl pyrazolone 4-ethyl-thiosemicarbazones compounds: 1-Phenyl-3-methyl-4-(4-bromo)benzal-pyrazol-5-one N(4)-ethyl-thiosemicarbazone (PM4Br BP-ETSC), 1-Phenyl-3-methyl-4-(4-methyl)benzal-pyrazol-5-one N(4)-ethyl-thiosemicarbaz -one (PM4MBP-ETSC), 1-Phenyl-3-methyl-4-benzal-pyrazol-5-one N(4)-ethyl-thiosemicarba -zone, 1,3-diphenyl-4-benzal-pyrazol-5-one N(4)-ethyl-thiosemicarbazone and 1-Phenyl-3-methyl-4-phenylacetyl-pyrazol-5-one N(4)-ethyl-thiosemi -carbazone have been synthesized and characterized by elemental analyses, IR, 1H NMR spectra and single-crystal XRD.

第一部分合成了五个4-酰基吡唑啉酮缩4-乙基-氨基硫脲化合物：1-苯基-3-甲基-4-（4-溴）苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲(PM4BrBP-ETSC)，1-苯基-3-甲基-4-(4-甲基)苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲(PM4MBP-ETSC)，1-苯基-3-甲基-4-苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲，1，3-二苯基-4-苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲和1-苯基-3-甲基-4-苯乙酰基-5-吡唑啉酮缩4-乙基-氨基硫脲，其中前四个具有光致变色性质。

At 60 ℃ the reaction of 1-O-alkyl-2-O-acetyl-3-O-trityl glycerol with iodine/methanol system removed trityl and acetyl and gave 1-alkyl glycerol. But at r.t. the reaction only removed trityl and gave two isomers 1-O-alkyl-2-O-acetyl glycerol and 1-O-alkyl-3-O-acetyl glycerol.

1-烷氧基-2乙酰氧基-3-三苯甲氧基甘油醚与碘/甲醇体系反应，在60 ℃时，同时发生了脱三苯甲基及乙酰基，在室温下，仅脱三苯甲基，但乙酰基在反应过程中发生了部分转移，产生了两个异构体。

Bromo-5-formyl -3-methylpyrrole is an important intermediate of tolyporohin. On the base of introducing the present research and development of tolypo- rohin and pyrroles ramification at home and abroad, an emphasis was made on synthesis of 2-Bromo-5-formyl -3-methylpyrrole and the technical conditions of all steps, which was described as follows. Diethyl 3,5-dimethylpyrrole-2,4-dicarboxylate was made by nitrification, reduction and cycle of ethyl acetoacetate.

由于2-溴-5-甲酰基-3-甲基吡咯是合成托尼卟吩的重要中间体，本文在阐述了当前托尼卟吩及吡咯衍生物的国内外研究和开发的基础上，重点研究了2-溴-5-甲酰基-3-甲基吡咯的合成，并对各步反应进行了工艺研究，具体合成步骤如下：本文通过对乙酰乙酸乙酯的亚硝化、还原、成环，反应生成吡咯单环衍生物2，4-二乙氧羰基-3，5-二甲基吡咯。

And Pharaoh spoke to Joseph, saying, Your father and your brothers have come to you.

47：5 法老对约瑟说，你父亲和你弟兄们到你这里来了。

Additionally, the approximate flattening of surface strip using lines linking midpoints on perpendicular lines between geodesic curves and the unconditional extreme value method are discussed.

提出了用测地线方程、曲面上两点间短程线来计算膜结构曲面测地线的方法，同时，采用测地线间垂线的中点连线和用无约束极值法进行空间条状曲面近似展开的分析。