氟苯

The trifluoromethyl modified benzofuran compounds synthesized by the invention contain a plurality of functional groups in benzene ring portion, and can be used as precursor for subsequent synthesis of benzofuran medicine intermediate containing trifluoromethyl.

本发明合成的三氟甲基修饰的苯并呋喃类化合物，苯环部分包括多种官能团，可以作为后续合成含三氟甲基苯并呋喃药物中间体的前体。

Ophenyl phenol,ophenyl phenol sodium salt tetrahydrate,7ADCA,2ethyl phenyl hydrazine hydrochloride,2,3dihydrofuran,7ethyl3(2hydroxy ethyl)indole,methyl ester of etodolac; 1,8diethyl1,3,4,9tetrahydropyrano[3.4b] indole1acetic acid methyl ester,5chloro2methoxy benzoic acid,4(2aminoethyl)benzene sulfonamide,5cyano phthalide,phthalhydrazide,9thioxanthenone,n[(1,4benzodioxane2yl)carboxyl]piperazine HCL,2chloro4amino6,7dimethoxyquinazoline,2chloro benzimidazole,1(4fluorobenzyl)2chlorobenzimidazole,2methylthio4pyrimidone,5amino4imidazole carboxamide HCL,6chloro2hexanone,11oxo6.11hydrodibenzothiepin,6,11dihydrodibenzooxepin11one,10,11dihydrodibenzocyclohepten5one;dibenzosuberone,dibenzo cyclohepten5one;dibenzosuberenone,3,5dihydroxy benzoic acid,3,5dihydroxy benzyl alcohol,2mercapto benzimidazole,3,4dihydroxy benzaldehyde,3,4dihydroxy benzonitrile,2amino5chloro benzonitrile,2(4chlorophenoxy)ethyl chloride,2(4chloro phenoxy)tert,butane,ditrimethylol propane;DTMP,2,2bis(4hydroxyphenyl)butane; bisphenol B,1,1'bis(4hydroxyphenyl)cyclohexane;bisphenol Z,tetrabromobisphenolS,3,5ditertbutyl salicylic acid,3,4,5trihydroxy benzoic acid stearyl ester,1,2,4trimethoxybenzene.

华业公司产品：邻苯基苯酚，邻苯基苯酚钠盐，7氨基3去乙酰氧基头孢烷酸，邻乙基苯肼盐酸盐，2，3二氢呋喃，7乙基色氨醇，依托度酸甲酯，5氯2甲氧基苯甲酸，4(2氨乙基)苯磺酰胺，5氰基苯酞，双酮酞嗪，9噻吨酮，N〔(1，4苯并二恶烷2基)羰基〕哌嗪盐酸盐，2氯4氨基6，7一二甲氧基喹唑啉，2氯苯并咪唑，1(4氟苄基)2氯苯并咪唑，2甲硫基4嘧啶酮，5氨基咪唑4 甲酰胺盐酸盐，6氯2已酮，11氧6.11二氢苯并〔b.c〕虑平，11氧代6，11二氢二苯并氧杂卓，10，11二氢二苯并环庚烯5酮，二苯并环庚烯5酮，3，5二羟基苯甲酸，3，5二羟基苯甲醇，2巯基苯并咪唑，3，4二羟基苯甲醛，3，4二羟基苯腈，2氨基5氯苯腈，2(4氯苯氧基)1氯乙烷，2(4氯苯氧基)叔丁烷，双丙烷，2，2二(4羟基苯基)丁烷；双酚B，1，1'双(4羟基苯基)环己烷；双酚Z，2[3，5二溴4(2，3二溴丙氧基)]苯砜，3，5二叔丁基水杨酸，3，4，5三羟基苯甲酸十八烷基脂，1，2，4三甲基氧基苯。

Suitable water-immiscible organic solvents include aromatic hydrocarbons, eg toluene, xylene, naphthalene, tetrahydronaphthalene and methyl naphthalene; chlorinated aromatic hydrocarbons, eg chlorobenzene, fluorobenzene, chloronaphthalene and bromonaphthalene; esters, eg butyl acetate, ethyl acetate, methyl benzoate, ethyl benzoate, benzyl benzoate, butyl benzoate, phenylethyl acetate, butyl lactate, benzyl lactate, diethyleneglycol dipropionate, dimethyl phthalate, diethyl phthalate, dibutyl phthalate, di(2-ethylhexyl) phthalate; alcohols having six or more carbon atoms, eg hexanol, octanol, benzyl alcohol, phenyl ethanol, phenoxy ethanol, phenoxy propanol and phenoxy butanol; ethers having at least 5 carbon atoms, preferably C 5-14 ethers, eg anisole and phenetol; nitrocellulose, cellulose ether, cellulose acetate; low odour petroleum distillates; turpentine; white spirits; naphtha; isopropylbiphenyl; terpene; vegetable oil; mineral oil; essential oil; and natural oil; and mixtures of any two or more thereof.

适用于水互溶的有机溶剂包括芳香族碳氢化合物，如甲苯，二甲苯，萘，四氢萘和甲基萘；氯代芳香族碳氢化合物，如氯苯，氟，氯萘和萘；酯类，如醋酸丁酯，醋酸乙酯，苯甲酸甲酯，苯甲酸乙酯，苄酯，苯甲酸正丁酯，苯，醋酸丁酯乳酸，乳酸苄，二甘醇二丙酸酯，邻苯二甲酸二甲酯，邻苯二甲酸二乙酯，邻苯二甲酸二丁酯，二（2乙基己基）酯；醇有6个或更多碳原子，如己醇，辛醇，苯甲醇，苯乙醇，苯氧基乙醇，丙醇和苯氧基苯氧丁醇；醚至少有5个碳原子，最好荤5-14醚，如苯甲醚和phenetol；硝化棉，纤维素醚，醋酸纤维素，低气味石油蒸馏；松节油；白酒，石脑油isopropylbiphenyl；萜类，植物油，矿物油，挥发油；和天然油，以及任何两个或两个以上其混合物。

In part one, the reactions of some active fluorine-containing compounds such as 2, 2-dihydropolyfluoroalkanoic acids and ethyl 2-hydropolyfluoroalkenoates were studied and various fluorine-containing heterocyclic compounds were synthesized. Using 2, 2-dihydropolyfluoroalkanoic acids as the starting material, 4-fluoroalkyl quinolin-2-ols, 2- [ -1-hydropolyfluoro-1-alkenyl] -4H-3, 1-benzoxazin-4-ones, 1-aryl -4, 9-dihydro-3-fluoro-alkyl-1H-pyrazo [3, 4-b] quinolin-4-ones, 5-fluoroalkyl-12H-quin olino [2, 1-b] quinazolin-12-ones, 4-fluoroalkyl-1, 3-dihydro-1, 5-benzodiazepin-2-ones and 4-fluoroalkyl-2H-pyrido [1, 2-a] pyrimidin-2-ones were synthesized through its condensation reaction with anilines, anthranilic acid, N'-aryl-o-aminobenzamides, o-nitro aniline, o-amino pyridine and their derivatives and the subsequent transformations. 5-Fluoroalkyl isoxazolidines, 3-fluoro-3-fluoroalkylisoxazolidino [4, 3-c] quinolin-4-ones, 3-fluoroalkylisoxazolino [4, 3-c] quinolin-4-ones and 2-aryl-3per fluoroacylindoles were synthesized by inter-and intramolecular 1, 3-dipolar cycloaddition of fluorine-containing olefins and nitrones.

第二部分，我们研究了α，α-二氟苄基卤类化合物的亚磺化脱卤反应、产物的转化及全氟烷基亚磺酸盐与芳环化合物的全氟烷基化反应，发现全氟苄基碘或溴及α，α一二氟苄基溴在保险粉等亚磺化脱卤试剂引发下可生成相应的亚磺酸盐；全氟苄基亚磺酸盐与氯气或溴反应可生成全氟苄基磺酰氯或磺酰溴；在烯烃存在下，全氟苄基碘则与烯烃发生加成反应，生成相应的1：1加成产物；在三价醋酸锰的作用下，部分芳香化合物如茴香醚，二甲氧基苯，吡啶，喹啉等可以和过量的全氟烷基亚磺酸盐发生双全氟烷基化反应，反应表现出一定的区域选择性，产率良好。

A series of crosslinked sulfonated polys were synthesized from 4,4'-difluorodiphenyl sulfone, 4,4'-biphenol, 3,3'-disulfonate-4,4'-difluorodiphenyl sulfone and 1,3,5-trihydroxy benzene by nucleophilic substitution polycondensation reactions. The trifunctional crosslinker of THB was in the mass fraction range of 3%-7%.

以4，4'-二氟二苯砜、4，4'-联苯二酚、3，3'-二磺化－4，4'-二氟二苯砜二钠盐和三羟基苯为原料，经高温溶液缩聚反应，制备了一系列不同磺化度的新型交联磺化聚芳醚砜。

In this thesis, we did modifications of alkyl groups upon benzyl fluorophosphonate. In order to study the influence of alkyl length and steric effect on activity and selectivity of probes, we synthesized benzyl fluorophosphonate recognition heads with modifications including ethyl, butyl, octyl and cyclohexyl. By way of connecting different kinds of tag like azido group, biotin and rhodamine with recognition heads separately through a higher hydrophilic ethylene glycol derived linker, a series of benzyl fluorophosphonate probes were made up. And they will apply to various biological testing strategies.

在本论文中，我们以苯甲基氟化磷酸酯为基础，於其上进行一系列烷基之修饰，为了探讨烷基长度与空间立体性质对於探针活性及选择性的影响，我们合成了包含乙烷基、丁烷基、辛烷基以及环己烷基修饰的苯甲基氟化磷酸酯辨识端，并藉由具较高亲水性的聚乙二醇衍生连接桥结合三种不同的发报端，分别有叠氮基团、生物素及萤光基团来构成不同的化学探针组合，这一系列苯甲基氟化磷酸酯类化学探针将可被应用於不同的生物测试策略。

1 Mol % dibenzoyl peroxide as catalyst and CCl_4 as solvent to give α-chloro-4-fluoro-3-phenoxybenzaldehyde and α,α-dichloro-4-fluoro-3-phenoxybenzaldehyde.

研究和优化了以4-氟-3-苯氧基甲苯为起始原料，经氯化反应，氧化反应合成对氟间苯氧基苯甲醛的方法。

The method comprises following steps: taking diphenol and 3- trifluoromethyl- 4- chloronitrobenzene as raw material, salt precipitating for diphenol and potash, refluxing with water- containing toluene, reacting with 3- trifluoromethyl- 4- chloronitrobenzene and getting dinitro monomer; taking dinitro monomer, ferro powder and HCl as raw material, ethanol and water as disslovant for refluxing and ethanol recrystallization, getting fluorine- containing aromatic diamido monomer.

合成方法是以二酚与3-三氟甲基-4-氯硝基苯作原料，先将二酚与碳酸钾成盐，甲苯带水回流反应，然后与3-三氟甲基-4-氯硝基苯反应制得二硝基单体；再以二硝基单体，铁粉，HCl为原料，乙醇和水做溶剂，回流反应、乙醇重结晶，得到含氟芳香二胺基单体。

To synthesize the octreotide, Phe-Leu-Glu-Glu-Leu and C_(15)H_(31)-CO-Lys-Thr -Thr-Lys-Ser peptides, the strategies are as followings: Fmoc- group as protective group for α-NH_2; TBTU, DIEA and HOBt as coupling reagent; and ethanedithiol -phenol - thioanisole - H_2O - TFA ( 2.5:5:5:5:82.5 , V/V ) as cleaving solution.

采用Fmoc固相合成法，以苯并三哗四甲基脲四氟硼酸盐、二异丙基乙胺和1-羟基苯骈三氮唑为缩合剂；苯酚—乙二硫醇—苯甲硫醚—水—三氟乙酸(5：5：2.5：5：82.5，V/V)为切割试剂，合成了奥曲肽、Phe-Leu-Glu-Glu-Leu及C_(15)H_(31)-CO-Lys-Thr-Thr-Lys-Ser三种小分子多肽，并对奥曲肽的合成规模进行了放大。

The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene. The latter is hydrolysed via 2,4-dichloro-5-fluoro-3-dichloromethylbenzoic acid, which can be isolated if necessary, to give 2,4-dichloro-5-fluoro-3-formyl-benzoic acid, the aldehyde group of which is reacted to give 2,4-dichloro-5-fluoro-3-N-hydroxyiminomethyl-benzoic acid, from which, with simultaneous conversion of the carboxyl group into the chlorocarbonyl group, water is eliminated using an acid chloride to give the nitrile 2,4-dichloro-3-cyano-5-fluoro-benzoyl chloride.

随后，在游离基条件下进行侧链的氯化，得到2，4-二氯-5-氟-3-二氯甲基-1-三氯甲基苯、后者被水解，经过2，4-二氯-5-氟-3-二氯甲基苯甲酸(如果需要此化合物可以分离)，得到2，4-二氯-5-氟-3-甲酰苯甲酸，将其醛基反应，得到2，4-二氯-5-氟-3-N-羟基亚氨基甲基苯甲酸，用酰氯从其中除去水，同时将羧基转化为碳酰氯，得到一种腈，即2，4-二氯-3-氰基-5-氯-苯甲酰氯。

The labia have now been sutured together almost completely.The drains and the Foley catheter come out at the top.

此刻阴唇已经几乎完全的缝在一起了，排除多余淤血体液的管子和Foley导管从顶端冒出来。

To get the business done, I suggest we split the difference in price.

为了做成这笔生意，我建议我们在价格上大家各让一半。