Abstract:
The present invention relates to a novel, high-yield and low-cost method for preparing entecavir, [1-S-(1α,3α,4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one, an antiviral agent, and novel intermediates used therein.
Abstract:
1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.
Abstract:
Provided is a method of preparing a (6R)-3-hexyl-4-hydroxy-6-undecyl-5,6-dihydropyran-2-one, and a (5R)-2-hexyl-5-hydroxy-3-iminohexadecanoate derivative used in said method as an intermediate.
Abstract:
The present invention relates to a method for preparing montelukast, an inhibitor against leukotrienes, and an intermediate used therein. According to the inventive method, high-purity montelukast or its sodium salt can be prepared in a high yield.
Abstract:
3R-carboxylate enantiomer derivative of formula (III) can be prepared easily and selectively by the method of the present invention, and a highly pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose derivative can be prepared efficiently from the compound of formula (III) as an intermediate.
Abstract:
A 3-(Z)-propenyl cephem compound is selectively prepared by reacting a phosphoranylidene cephem compound with acetaldehyde in the presence of a base in a solvent mixture comprising diethyl ether, formula (I), wherein R is a carboxyl protecting group; R1 is hydrogen or R2CH2CO—; and R2 is ethyl, 2-thiophenyl, phenyl, p-hydroxyphenyl or phenoxy
Abstract translation:通过在碱存在下将亚正膦基头孢烯化合物与乙醛反应在包含二乙醚,式(I)的溶剂混合物中,其中R是羧基保护基,选择性地制备3-(Z) - 丙烯基头孢烯化合物。 R 1是氢或R 2 CH 2 CO-; R 2是乙基,2-噻吩基,苯基,对羟基苯基或苯氧基
Abstract:
A method for preparing a 1-androstene derivative which comprises reacting a 2-iodo-androstane derivative with an oxidizing agent while maintaining the pH of the reaction mixture at a specific range gives the 1-androstene derivative with high purity and yield.
Abstract:
A flameproof thermoplastic resin composition of the present invention comprises (A) a base resin comprising 40 to 95% by weight of a rubber modified styrene-containing resin (a1) composed of 20 to 100% by weight of a styrene-containing graft copolymer resin (a11) and 0 to 80% by weight of a styrene-containing copolymer resin (a12), and 60 to 5% by weight of polyphenylene ether resin (a2); (B) 2 to 40 parts by weight of a styrene-acrylonitrile copolymer containing 5 to 18% by weight of acrylonitrile per 100 parts by weight of the base resin; (C) 5 to 30 parts by weight of an aromatic phosphoric acid ester compound having a melting point of more than 90° C. per 100 parts by weight of the base resin; and (D) 3 to 30 parts by weight of a phenolic resin per 100 parts by weight of the base resin. The flameproof thermoplastic resin composition may further comprise 0 to 30 parts by weight of an anti-dripping agent, an impact modifier, a plasticizer, a heat stabilizer, an oxidation inhibitor, a light stabilizer, a compatibilizer, pigments, dyes and/or inorganic fillers on the basis of 100 parts by weight of the base resin.
Abstract:
Highly pure cefpodoxime proxetil can be prepared by a simple process comprising the step of reacting a cefpodoxime salt with 1-iodoethylisopropylcarbonate in an organic solvent in the presence of a crown ether.
Abstract:
The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.