52 results about "Haloketone" patented technology

A method is provided for synthesizing acylamides, useful as protectant for cultivated plants. A benzoxazine, such as 3,4-dihydro-3-methyl-2H-1,4-benzoxazine, is made in a stepwise manner by initially forming an o-nitrophenoxyketone by reacting a haloketone and a nitrophenol. The o-nitrophenoxyketone is hydrogenated to form the corresponding benzoxazine, which is thereafter acylated with an acylhalide to produce the acylamide, such as 4-dichloroacetyl-3,4-dichloroacetyl-3,4-dihydro-3-methyl-2H-1,4-benzoxazine.

The S-DABO compound, its synthesis method and application belong to the technical field of medicine. The invention relates to a 5-alkyl-6-phenyl-2-(substituted arylcarbonylmethylthio)uracil compound, which has the following general formula: wherein: R1 is a C1-3 alkyl group; R2=C1-6 alkyl, substituted furan ring, thiophene ring, benzene ring (substituents on the aromatic ring are H, OH, C1-3 alkoxy). The product of the present invention is obtained by reacting 5-alkyl-6-phenylthiouracil with a-halogenated ketone under K2CO3 catalysis. The synthesis method is simple and easy, and the product has significant anti-HIV virus activity, low toxicity and high selectivity index, and can be used as a candidate anti-HIV drug.

Alpha-haloketones are useful alkylating agents for coupling to sulfhydryl-containing biomolecules. However, they react spontaneously with water, alkali and organic bases and therefore cannot be stored for extended periods of time in aqueous solutions, particularly in the presence of proteins at physiological pH. The present invention provides novel solutions to these problems, however, as novel compounds and compositions comprising protected haloketones are disclosed herein. Methods of preparing and using protected haloketones which are useful in a variety of applications-e.g., in assays and conjugation reactions-are also disclosed herein.

The present invention relates to a pyridin-2-one compound and a preparation method thereof, in particular to a substituted pyridin-2-one compound and a preparation method thereof. The method mainly solves the technical problems that the existing pyridin-2-one compound derivatives are few and the synthesis methods are few. The technical scheme of the present invention is: a substituted pyridin-2-one compound, the general structural formula is as follows:, Formula 1; wherein R1 is hydrogen, a straight-chain alkyl group with 1 to 6 carbon atoms, and a side chain containing a substituent One of alkyl, substituted aryl, substituted benzyl or a-haloketone. R2 is one of hydrogen, a straight-chain alkyl group with 1 to 6 carbon atoms, an alkyl group containing a substituent side chain, a substituted aryl group or a substituted benzyl group.

The invention discloses a method for synthesizing a 1, 4-diketone compound without a catalyst. In the existence of alkali, the corresponding 1, 4-diketone compound is obtained by reacting silyl enol ether and alpha-haloketone by taking perfluoroalkyl alcohol as a solvent. By adopting the method for synthesizing the 1, 4-diketone compound, the raw materials are easily obtained, the cost is low, the reaction conditions are mild, the operation is simple and easy to control, the side reactions are few, the after-treatment is simple, the product yield is relatively high, and the solvent can be recovered and recycled, so that the production cost is greatly saved; the method has good environment protection benefit and economical benefit and is suitable for industrial large-scale production.

The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxy alcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.

The present invention relates to a novel process for the synthesis of the intermediate compounds constituted by chromanyl haloketones of formula III and 6-fluoro-2-(oxiran-2-yl)chromans of formula I.The intermediates thus obtained can be used for the synthesis of Nebivolol.

The present invention provides an improved process for the preparation of methyl-methyl-3,4-dihydro-2H-pyran-5-carboxylate of formula (IV), comprising the steps of: (IV) (i) alkylating 1-Bromo-3-chloropropane of formula (I) with Methylacetoacetate of formula (II) to prepare haloketone of formula (VII) in presence of an alcoholic solvent; (I) (II) (VII) (ii) O-alkylating the compound of formula (VII) with sodium methoxide to obtain the desired molecule methyl-methyl-3,4-dihydro-2H-pyran-5-carboxylate of formula (IV) in its crude form; (VII) (IV) (iii) Purifying the content of step (ii) above by fractional distillation to obtain the purified molecule of formula (IV).

The invention relates to a novel method for asymmetric syntheses of (R)-salbutamol hydrochloride by using a high-efficiency chiral catalyst. The method comprises the following steps: 1) subjecting salicylaldehyde and halogenoacetyl halide to Friedel-Crafts acylation so as to obtain halogenated ketone; 2) subjecting the obtained halogenated ketone to aminolysis with tert-butylamine and then carrying out hydrolysis and deprotection so as to obtain salicylaldamino ketone; and 3) reducing the salicylaldamino ketone into a crude product of (R)-salbutamol in the presence of a chiral borane catalyst derived from chiral aminoalcohol and carrying out purification and salt formation of hydrochloric acid so as to obtain the high purity (R)-salbutamol hydrochloride.