Abstract:
Enolate salts of 4-fluoro-2-hydroxymethylene-3-oxobutyrates of formula wherein R1 is C1-10 alkyl, R2 and R3 are independently hydrogen or fluorine, M is an alkali or alkaline earth metal, and n is 1 or 2, are prepared from enolate salts of the corresponding 4-fluoro-3-oxobutyrates and carbon monoxide. The enolate salts of formula I can be alkylated or acylated to obtain the corresponding enol ethers and esters. The 4-fluoro-3-oxobutyrate starting material can be prepared from 1,1-difluoroethyl methyl ethers by SbF5-catalyzed fluoromethane elimination followed by halogen exchange with lithium chloride, reacting the thus obtained fluoroacetyl chloride with ketene and quenching with the appropriate alcohol R1-OH.
Abstract:
Hydroxy acid compound of substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), Y = C 1-4 straight carbon chain. The compound can release 2, 6-diisopropylphenol rapidly under the action of enzymes in vivo, which has sedative, hypnotic and/or anesthetic effect. By protecting the hydroxyl group of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis, and/or anesthesia.
Abstract translation:提供取代苯基酯的羟基酸化合物,其制备方法和医疗用途。 标题化合物如式(I)所示,Y = C 1-4直链碳链。 该化合物可在体内酶的作用下快速释放2,6-二异丙基苯酚,具有镇静,催眠和/或麻醉作用。 通过保护式(I)化合物中2,6-二异丙基苯酚的羟基,2,6-二异丙基苯酚的首过代谢活性降低,合成化合物可用于镇静,催眠和/或 麻醉。
Abstract:
A rosuvastatin calcium intermediate as shown by Formula I is prepared as follow: a) subjecting chloroethylene, magnesium and R-epoxy chloropropane to Grignard reaction, b) adding sodium cyanide for nucleophilic substitution reaction, c) adding alcohol for alcoholysis reaction, d) adding alkaline solvent for hydroxyl protection, e) subjecting the mixture to oxidation reaction, f) adding triphenyl phosphorus and subjecting to Wittig reaction in the presence of alkali to obtain the compound of formula I. The method has moderate reaction conditions, is convenient and stable and can be applied to industrial production.
Abstract:
The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.
Abstract:
The present invention concerns a method for the preparation of therapeutically valuable triphenylbutene derivatives, especially ospemifene or fispemifene. formula (I).
Abstract:
The present invention provides a cooling component or sensate component which has further strong cooling intensity and is excellent in the persistency or refresh-feeling and cool-feeling, a sensate composition comprising the same, and various products comprising the sensate composition. The present invention relates to, as a cooling component or sensate component, (3R)-1-menthyl 3-hydroxybutyrate represented by the following formula (I):
Abstract:
The present invention relates to a process for preparing a compound of formula (IV)
where W is the methyl ( E )-2-(3-methoxy)acrylate group, which comprises the steps of: (i) reacting the compound of formula (IV) where W is the methyl 2-(3,3-dimethoxy)propanoate group with a reagent that will protect the hydroxyl group of that compound from reaction during subsequent demethanolysis; (ii) eliminating methanol from the hydroxyl-protected compound formed in step (i); and (iii) removing the hydroxyl-protecting group formed in step (i) to form a compound of formula (IV) where W is the methyl ( E )-2-(3-methoxy)acrylate group.
Abstract:
A method is provided for producing an ester-substituted phenol product stream from an ester-substituted diaryl carbonate manufacturing waste stream. The method includes the steps of obtaining a waste stream containing an ester-substituted diaryl carbonate from an ester-substituted diaryl carbonate manufacturing facility and creating a reaction mixture by combining the waste stream with a solvent and with a transesterification catalyst. The reaction mixture is maintained at a reaction pressure at or below atmospheric pressure, and at a reaction temperature for a period of time sufficient to produce ester-substituted phenol by solvolysis of the ester-substituted diaryl carbonate. Ester-substituted phenol is removed from the reaction mixtures in an ester-substituted phenol stream. The solvent, the reaction temperature, and the reaction time are selected in combination such that less than 1,000 ppm of acid-substituted phenol is present in the ester-substituted phenol stream.
Abstract:
[PROBLEMS] A process for obtaining 6,7-bis(2-methoxyethoxy)quinazolin-4-one in a high yield from ethyl 2-amino-4,5bis(2-methoxyethoxy)benzoate. [MEANS FOR SOLVING PROBLEMS] The process for producing 6,7-bis(2-methoxyethoxy)quinazolin-4-one comprises reacting ethyl 2-amino-4,5-bis(2-methoxyethoxy)benzoate with a formic acid compound in the presence of an ammonium carboxylate.