烯基

This invention provides compounds of Formula; wherein: R is a moiety selected from the group: and n is an integer of 1 or 2; R is selected from hydrogen, amino,-NRR, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, alkynyl of 2 to 12 carbon atoms optionally substituted, halogen, and a 5 to 10 membered heteroaryl ring optionally substituted, having 1 to 4 heteroatoms independently selected from N, O and S; R is selected from hydrogen, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, vinyl, alkynyl of 2 to 12 carbon atoms optionally substituted and halogen; R is H, alkyl of 1 to 12 carbon atoms optionally substituted, cycloalkyl of 3 to 8 carbon atoms, bicycloalkyl of 5 to 10 carbon atoms or aralkyl optionally substituted; R is OH or -OH; R and R are each independently H or alkyl of 1 to 12 carbon atoms or when optionally taken together with the nitrogen atom to which each is attached form a 3 to 8 membered saturated heterocyclyl ring; R is alkyl of 1 to 12 carbon atoms optionally substituted; or a tautomer or pharmaceutically acceptable salts thereof.

本发明提供式的化合物；其中：R 1 为选自基团和的部分；n为整数1或2；R 2 选自氢、氨基、-NR 6 R 7 、具有1到12个碳原子的视情况经取代的烷基、具有6个、10个或14个碳原子的视情况经取代的芳基、具有2到12个碳原子的视情况经取代的烯基、具有2到12个碳原子的视情况经取代的炔基、卤素和具有1到4个独立地选自N、O和S的杂原子的视情况经取代的5元到10元杂芳基环；R 3 选自氢、具有1到12个碳原子的视情况经取代的烷基、具有6个、10个或14个碳原子的视情况经取代的芳基、具有2到12个碳原子的视情况经取代的烯基、乙烯基、具有2到12个碳原子的视情况经取代的炔基和卤素；R 4 为H、具有1到12个碳原子的视情况经取代的烷基、具有3到8个碳原子的环烷基、具有5到10个碳原子的双环烷基或视情况经取代的芳烷基；R 5 为OH或-OH 8 ；R 6 和R 7 各自独立地为H或具有1到12个碳原子的烷基，或当视情况与其所连接的氮原子连接在一起时形成3元到8元饱和杂环基环；R 8 为具有1到12个碳原子的视情况经取代的烷基；或其互变异构体或医药学上可接受的盐。

ABSTRACT Immobilized penicillin acylase (from E.coli) was used to catalyze 7 phenylacetamido 3 E propenyl cephalosporanic acid hydrolyzation into 7 amino 3 E propenyl cephalosporanic acid. Then, trans APRA was acylated with hydroxyethyl ester of 4 hydroxy D phenylglycine to obtain trans cefprozil.

以7 苯乙酰氨基 3 E 丙烯基 3 头孢菌素 4 羧酸为原料，在青霉素酰化酶作用下，首先酶法水解得到3 E 丙烯基 3 头孢菌素 4 羧酸，过滤固相酶，滤液调pH分离得到反式APRA固体；在青霉素酰化酶作用下，反式APRA再与对羟基苯甘氨酸乙二醇酯缩合，得到反式头孢丙烯；酶法合成所得的产品与进口反式头孢丙烯对照品一致。

Analysis of the material change, garlic cells bioactive aliphatic thio cysteine sulfoxide and thiosulfate propenyl cysteine sulfoxide sulfur compounds in garlic, such as the role of enzymes, the generation of thiobarbituric acid sub - ester, propylene-based thiosulfinates, allyl thiosulfinates as garlic pigment precursor substances, and further changes occurred in the green garlic.

从物质变化分析，大蒜细胞中的生物活性物质硫代脂肪族半胱氨酸亚砜和硫代丙烯基半胱氨酸亚砜等含硫化合物在蒜酶的作用下，生成硫代亚磺酸酯、丙烯基硫代亚磺酸酯、烯丙基硫代亚磺酸酯，作为大蒜色素物质的前体，进一步发生大蒜绿变。

Chapter three: The studies of zinc dust assisted the green carbonyl olefination under thesolvent-free conditions.

第三章：锌粉促进无溶剂下羰基化合物的绿色烯基化反应研究该部分首次研究了在TMSiCl存在下，无溶剂非催化条件下，锌粉促进溴化苄与羰基化合物的烯基化反应，发现在无溶剂锌粉促进下，可以将羰基化合物立体选择性

New sulfonyloxadiazolones have the formula, in which A stands for hydrogen, sulphur,-SO-,-SO2- or a group, in which R stands for hydrogen or alkyl; R stands for optionally substituted cycloalkyl, cycloalkenyl or aryl; and R stands for optionally substituted alkyl, alkenyl, dialkylamino or aryl.

本发明涉及式新的磺酰基__二唑酮，其中，A代表氧、硫、－SO－、－SO 2 －或基团，其中R 3 代表氢或烷基；R 1 代表任选被取代的环烷基，任选被取代的环烯基或任选被取代的芳基；和R 2 代表任选被取代的烷基，链烯基，二烷基氨基或芳基。

The dissertation mainly consists of two parts:1. The Reaction Chemistry of Alkynes under Palladium Catalysis Part 1 studies the reaction α,β-unsaturated carbonyl compounds with alkenylpalladium intermediate generated by nucleopalladation, and discovered 1 the Pd-catalyzed tandem addition reaction of halides, alkynes and α,β-unsaturated carbonyls,2 the four-component tandem addition reaction of halides, alkynes and α,β-unsaturated carbonyls, 3 the tandem intramolecular oxypalladation-conjugate additionreaction of alkynoic acids with α,β-enals. These new reactions provide notonly efficient highly stereoselective methods for the synthesis of γ,δ-unsaturated,polyunsaturated carbonyl compounds and γ-lactonic aldehydes, but also thebasic transformations for a number of C-C bond formation reactions which can be usedto design synthesis of many acyclic, cyclic or polycyclic compounds.

本论文的主要工作分为两个部分：一、钯催化下炔烃的反应化学在本小组前人工作的基础上，我们详细研究了炔烃亲核钯化产生的烯基钯中间体与α，β-不饱和羰基化合物的反应，发现两价钯催化下卤离子-炔烃-α，β-不饱和醛酮的串联加成反应、卤离子-炔烃-α，β-不饱和醛酮的西组分串联加成及炔酸分子内氧钯化-串联Michael型加成反应；由此发展了γ，δ-不饱和醛酮、多不饱和羰基化合物和带有醛酮基侧链的γ-丁内酯衍生物的高立体选择性合成方法，这一过量卤离子存在下的烯基钯对α，β-不饱和羰基化合物共轭加成反应的发现，为大量碳-碳键形成反应的实现提供了基础，使我们能够从这一基本反应出发，设计和开发多种分子内、分子间的碳碳成键反应，以好的立体、区域选择性组建开链、环状及多环类型的化合物。

That 1,4-addition reactions of Grignard agent made from 1-bromo-3-triphenylmethoxyl-1-octene and organozinc agent made from 1-iodo-3-trimethysiloxy-1-octene with 2-(6-methoxylcarbonylhexyl)-4-(2- tetrahydro-pyranyloxy)-2-cyclopentenone both gave prostaglandin 〓 methyl ester statethat prostaglandin E compounds can be prepared by 1,4-addition reaction oforganozinc agent.

最后，研究了溴化-3-三苯甲氧基-1-辛烯基镁和碘化-3-三甲硅氧基-1-辛烯基锌与2-(6-甲氧羰己基)-4-(2-四氢吡喃氧基)-2-环戊烯酮通过1，4-加成反应合成〓甲酯的方法，结果表明，用有机锌试剂通过1，4-加成反应来合成PGE类化合物是可行的。

The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C-,-O-C-,-NR8-C-,-O-C1-6alkanediyl-C-,-NR8-C1-6alkanediyl-C-,-S2-,-O-S2-,-NR8-S2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC, carboxyl, aminoC, mono- or di(C1-4alkyl)aminoC, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl.

本发明涉及右式化合物其N-氧化物、盐、立体异构形式、外消旋混合物、前药、酯及代谢物，其中R 1 及R 8 各是氢、C 1-6 烷基、C 2-6 烯基、C 3-7 环烷基、芳基、Het 1 、Het 2 ；R 1 也可以是式(R 11a R 11b )NC(R 10A R 10b )CR 9 -之基；t是0、1或2；R 2 是氢或C 1-6 烷基；L是-C-、-O-C-、-NR 8 -C-、-O-C 1-6 烷二基-C-、-NR 8 -C 1-6 烷二基-C-、-S 2 -，-O-S 2 -、-NR 8 -S 2 -；R 3 是C 1-6 烷基、芳基、C 3-7 环烷基、C 3-7 环烷基C 1-4 烷基或芳基C 1-4 烷基；R 4 是氢、C 1-4 烷基OC、羧基、氨基C、一-或二(C 1-4 烷基)氨基C、C 3-7 环烷基、C 2-6 烯基、C 2-6 炔基或任选被取代的C 1-6 烷基；R 5 及R 6 是氢或C 1-6 烷基。

Treatment of polystyrene-supported selenium ,bromide with lithium acetylides afforded polystyrene-supported selenoacetylene, which reacted with dicyclohexylborane giving a way for stereoselective synthesis of polymer-supported- vinylic selenides .

聚苯乙烯负载硒溴与炔基锂反应合成聚苯乙烯负载炔基硒醚，再与二环己基硼烷反应制得聚苯乙烯负载顺式烯基硒醚；此负载型烯基硒醚在NiCl2(PPh3)2存在下与格氏试剂发生偶联反应，提供了一种有效的-1，2-二取代乙烯的固相有机合成方法

In this project, we have prepared conveniently Si-Mg 1,1-difunctional group reagents-α-silylvinyl Grignard reagents by hydromagnesiation of alkynylsilanes; Se-Br 1,1-difunctional group reagents-α-bromovinylselenides by hydrobromination of alkynylselenides; Sn-Br and Sn-I 1,1-difunctional group reagents by hydrozirconation of alkynylstannanes followed by halogenating reaction.

本项目通过炔基硅烷的镁氢化反应，方便地制得了Si-Mg 1，1-双官能团试剂-α-硅基烯基镁化物；通过炔基硒醚的溴氢化反应，方便地制得了Se-Br 1，1-双官能试剂-α-溴代烯基硒醚；通过炔基锡烷的锆氢化反应，继而卤代方便地制得了Sn-Br和Sn-I 1，1-双官能试剂。

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。