甲酰化

Methods 4-Hydroxy- benzonitrile was treated with sodium hydrogen sulfide and anhydrous magnesium chloride in dimethyl formamide to give thioamide, which was then directly cyclized with ethyl 2-chloroacetoacetate without separation to give ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(2) in one-pot; then 2 was formylated with Duff reaction adopting hexamethylenetetramine in trifluoroacetic acid to give ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(3); finally, the target compound was obtained by the treatment of 3 with hydroxylamine hydrochloride and sodium formate in formic acid.

采用"一勺烩"方法，以4-羟基苯甲腈为起始原料，首先与硫氢化钠和无水氯化镁在N，N-二甲基甲酰胺中反应，所得中间体不经分离，直接加入2-氯乙酰乙酸乙酯进行环合反应，得到2-(4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（2）；然后通过六亚甲基四胺/三氟乙酸进行Duff反应，得到2-(3-甲酰基-4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（3）；再经盐酸羟胺/甲酸/甲酸钠体系脱水得到目标化合物。

Teflubenzuron was synthesized from 2,4-difluoronitrobenzene and 2,6-dichlobenil as starting reagent through six-step reaction with the yield of 75.3%.3,5-Dichloro-2,4-difluoroaniline was synthesized by chlorination,reduction reaction from 2,4-difluoronitrobenzene,the yield was 84.5%;2,6-difluorobenzamide with the yield of 87.7% was synthesized by fluoridation and hydrolysis from 2,6-dichlobenil.

以2，4-二氟硝基苯和2，6-二氯苯腈为起始原料，经过6步反应合成伏虫隆，总收率为75.3%。以2，4-二氟硝基苯为原料，经过氯化、还原反应合成3，5-二氯-2，4-二氟苯胺，产率为84.5%；以2，6-二氯苯腈为原料，经过氟化和水解，制得2，6-二氟苯甲酰胺，产率为87.7%；将Ⅱ与二碳酸酯酰化，合成2，6-二氟苯甲酰异氰酸酯，产率为91.3%；Ⅲ与Ⅰ加成，得到杀虫剂伏虫隆，产率为95%。

The better reaction conditions are as follows: Reaction temperature is 40°C, Reaction time is 5 hour; the ratio of L - phenylalanine to acetic acid and N - formyl - L- aspartyl anhydrideis 1:10.2:1.1, Its yield is 95.4%.

在查阅文献的基础上，得到较优的α-L-天冬氨酰L-苯丙氨酸甲脂盐酸盐的合成方案，在甲醇一水体系中，N-甲酰-α-L-天冬氨酰-L-苯丙氨酸在浓盐酸的作用下60℃水解90分钟，后冷却到15℃加入浓盐酸在20～30℃保温反应96小时，进行甲脂化，形成甲脂盐酸盐，结晶析出。

Three formyl group functional cross-linking polystyrene resins of p -formylphenoxymethyl, p -formyl-2-methoxphenoxymethyl,and p -formyl-3-methoxphenoxymethyl were facilely and rapidly synthesized from Merrifield resin under phase transfer catalytic condition coupling with microwave irradiation in a domestic microwave oven.

以Merrifield树脂为原料，家用微波炉为反应装置，在微波照射的相转移催化条件下，简便快速地合成了3种甲酰基功能化的交联聚苯乙烯树脂——对甲酰基苯氧基甲基树脂、对甲酰基-2-甲氧基苯氧基甲基树脂和对甲酰基-3-甲氧基苯氧基甲基树脂。

Three formyl group functional cross-linking polystyrene resins of methoxphenoxymethyl, and p-formyl-3-methoxphenoxymethyl were facilely and p-formylphenoxymethyl, p-formyl-2-rapidly synthesized from Merrifield resin under phase transfer catalytic condition coupling with microwave irradiation in a domestic microwave oven.

以Merrifield树脂为原料，家用微波炉为反应装置，在微波照射的相转移催化条件下，简便快速地合成了3种甲酰基功能化的交联聚苯乙烯树脂--对甲酰基苯氧基甲基树脂、对甲酰基-2-甲氧基苯氧基甲基树脂和对甲酰基-3-甲氧基苯氧基甲基树脂。

Results show that, by using thionyl chloride and N,N-dimethyl formamide as chlorinating reagent and dichloromethane as solvent and taking -15℃ as reaction temperature, Z-iomer crystals with pale white color and stable to temperature can be obtained with an overall yield of 70%.

以2-（2-氨基噻唑－4-基）－2-甲氧亚氨基乙酸为原料，经盐酸化、氯代等反应合成了Z-2-（2-氨基噻唑－4-基）－2-甲氧亚氨基乙酰氯盐酸盐；氯代时以用亚硫酰氯和N，N-二甲基甲酰胺的混合物代替五氯化磷作氯化剂，并考察了温度和溶剂对氯代产物中Z-异构体和E-异构体收率的影响。

They are, 4 21-amidohydrocortisone Ba1～Ba4, 10 21-amidoprednisolone Bb1～Bb10, 4 21-amidomethylprednisolone Bc1～Bc4, 4 21-amidodexamethasone Bd1～Bd4, 1 21-amidobetamethasone Be1, 1 21-amidoRS Bf1, 1 21-amidocortisone Bg1, 1 21-amidoprednisone Bh1. The amido groups were acetamido, nicotinamido, hemesuccinamido, benzoylamido, methanesufonamido, or arylsufonylamido.

包括：4个21-酰胺基氢化可的松（Ba1～Ba4），10个21-酰胺基氢化泼尼松（Bb1～Bb10），4个21-酰胺基甲泼尼龙（Bc1～Bc4），4个21-酰胺基地塞米松（Bd1～Bd4），1个21-酰胺基倍它美松（Be1），1个21-酰胺基RS（Bf1），1个21-酰胺基可的松（Bg1），1个21-酰胺基强的松（Bh1）。21-酰胺基分别为乙酰胺基、烟酰胺基、单琥珀酰胺基、苯甲酰胺基、甲烷磺酰胺基或取代苯磺酰胺基等。

METHODS: Based on the antitumor activity and structural feature of 8-chloroadenosine and retinoic acid, modifications were made at positions 5′ and 8,substituted cinnamoyl and benzoyl groups were bound at 8 position through amido and ester bonds, sulfonation and nitrosation at 5′-OH and its direct chlorination were conducted.

对腺苷的8位和8-Cl-腺苷的糖环羟基进行了结构改造，以酰胺键和酯键在腺苷的8位连接了具共轭基团的肉桂酰基和苯甲酰基，得到腺苷的维甲类似物；对8-Cl-腺苷的5′-羟基进行了甲磺酰化，硝基化以及氯代反应，得到了它的衍生物。

Methods 4-Hydroxy- benzonitrile was treated with sodium hydrogen sulfide and anhydrous magnesium chloride in dimethyl formamide to give thioamide, which was then directly cyclized with ethyl 2-chloroacetoacetate without separation to give ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(2) in one-pot; then 2 was formylated with Duff reaction adopting hexamethylenetetramine in trifluoroacetic acid to give ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(3); finally, the target compound was obtained by the treatment of 3 with hydroxylamine hydrochloride and sodium formate in formic acid.

采用&一勺烩&方法，以4-羟基苯甲腈为起始原料，首先与硫氢化钠和无水氯化镁在N，N-二甲基甲酰胺中反应，所得中间体不经分离，直接加入2-氯乙酰乙酸乙酯进行环合反应，得到2-(4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（2）；然后通过六亚甲基四胺/三氟乙酸进行Duff反应，得到2-(3-甲酰基-4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（3）；再经盐酸羟胺/甲酸/甲酸钠体系脱水得到目标化合物。

Methyl phenyl glyoxylate was prepared firstly by reaction of 2-methyl benzoyl chloride with NaCN. The reaction of 2-methyl phenyl glyoxylate with methanol gave the target product methyl 2-methyl phenyl glyoxylate. An improved 3 step synthetic method of methyl 2-methyl phenyl glyoxylate was studied. The optimization conditions were presented.

以2-甲基苯甲酸为原料，酰化后与氰化钠反应生成2-甲基苯甲酰腈，经甲酯化生成2-甲基苯甲酰甲酸甲酯，改进了三步合成2-甲基苯甲酰甲酸甲酯的方法，并对反应时间、反应温度等影响因素进行了优化，确定了合成反应中的最优化条件。

We have no common name for a mime of Sophron or Xenarchus and a Socratic Conversation; and we should still be without one even if the imitation in the two instances were in trimeters or elegiacs or some other kind of verse--though it is the way with people to tack on 'poet' to the name of a metre, and talk of elegiac-poets and epic-poets, thinking that they call them poets not by reason of the imitative nature of their work, but indiscriminately by reason of the metre they write in.

索夫农 、森那库斯和苏格拉底式的对话采用的模仿没有一个公共的名称；三音步诗、挽歌体或其他类型的诗的模仿也没有——人们把&诗人&这一名词和格律名称结合到一起，称之为挽歌体诗人或者史诗诗人，他们被称为诗人，似乎只是因为遵守格律写作，而非他们作品的模仿本质。

The relationship between communicative competence and grammar teaching should be that of the ends and the means.

交际能力和语法的关系应该是目标与途径的关系。