Abstract:
PURPOSE: The trifluoromethylketone derivatives supported on silica gel and a producing method thereof are provided to be used as a useful catalyst in the epoxidation reaction using olefin and Oxone oxidizing agent. CONSTITUTION: The trifluoromethylketone derivatives are represented by formula (3), in which R1 is C1 to C6 alkyl, R2, R3 and R4 are individually hydrogen or C1 to C6 alkyl, I is an integer from 0 to 1, m is methylene from 1 to 6, n is an integer from 0 to 2, and O is methylene from 0 to 16. The trifluoromethylketone derivatives of formula (3) supported on silica gel are produced by reacting trifluoromethylketone derivatives of formula (1) with mercaptoalkylsilanized silica gel of formula (2) in the presence of organic solvents such as azobisisobutyronitrile, benzene, toluene, acetonitrile or chloroform.
Abstract:
7- Acylamino-3-(5- methoxythiazolin-2-yl) thiomethyl-3-cephem carboxylic acid derivs. of formula(I) are new. In (I), R=H, 2- (2aminothiazol-4-yl)-2(syn)- methoxyiminoacetyl, 2-(2- aminothiazol - 4-yl)-2-(2-t- butoxycarbonyl-2- propyloxyimino) acetyl, 2- (2aminothiazol-4-yl)-2-(2-carboxy-2-propyloxyimino)acetyl or D(-) alpha-(4- ethyl-2,3- dioxo-1- piperazine carboxyamido)-alpha- (4hydroxyphenyl)acetyl; R'=H or paramethoxybenzyl (PMB). Also claimed is the prepn. of (I) which comprises cyclizing dithiocarbamate of formula (II) in acidic condition and acylating the obtd. intermediate with an acetate deriv.
Abstract:
5-Alkoxy-2-substd. thio-1,3-thiazoline derivs. of formula (I) are new. Also claimed is the prepn. of (I) which comprises a heat- transfer reaction of dithiocarbamate of formula (II) under the condition of 1-5 mmHg and 200 ± 10 deg.C or a cyclization-reaction of (II) under acidic condition. In the formulas, R=H, C1-6 alkyl, allyl, 2-propinyl, benzyl or 2- piridylmethyl; R1= methyl or ethyl. Pref. the acid is selected from trifluoroborane, anhydrous magnesium bromide or conc. H2SO4.
Abstract:
The method for preparing piperidine derivatives of formula (I) useful for the antihistaminic agent is presented. Thus, 37.7g of ethylisonipecotate, 35.0g of potassium hydrogen carbonate, 52.5g of 4-chloro-p-t-butylbutyropenone and a small amount of potassium iodine are added to 800ml of toluene and the above mixture is reacted for 24 hrs. The above reacted solution is cooled to room temperature and added with 300ml of water to the cooled solution. The obtained water layer is extracted with 300ml of toluene twice and the extract is dried.