Development Center for Biotechnology

Taigen Biotechnology Company, Ltd.

Taigen Biopharmaceuticals Co.(beijing), Ltd.

Shan-Yen Chou

Shyh-Fong Chen

Wen-Chang Chen

Chi-Feng Yen

Shan-Shue Wang

Hao Ku

Han-Pei Hsu

Tsai-Mien Huang

Chu-Chung Lin

Ming-Chu Hsu

Chi-Hsin Richard King

Chia-Lin J Wang

Chin-Fen Lee

Hsiao-Hwa Lu

Han-Jung Tsai

Shih-Chieh Chuang

Hou Ku

Wei-Kun Yin

Paw-Hwa Yang

Pei-Ling Lee

Provided is a stereoselective synthesis of an intermediate for the preparation of the heterocyclic derivative as a Cap-dependent endonuclease inhibitor. The synthesis process has the advantages of simple operation, higher yield and relatively controllable steroselectivity, such that it is suitable for large-scale production.

Stereoselective synthesis of intermediate for preparation of heterocyclic compound

A trans-isomeric compound of formula (I) below or a pharmaceutically acceptable salt thereof: in which Ris C-Calkyl or C-Ccycloalkyl and the trans-isomeric compound has a trans:cis ratio of at least 70:30. Further disclosed is a method for preparing the trans-isomeric compound.

Trans-isomeric heterocyclic compounds and preparation thereof

Disclosed are novel 1,2,4-triazin-5-one biphenyl derivatives having structural formula (I) useful as non-peptide antagonists of angiotensin II receptor: ##STR1## where R.sub.1 represents alkyl, cycloalkyl, or substituted or unsubstituted aryl;

Angiotensin II receptor antagonistic 1,2,4-triazin-5-one derivatives

A compound of formula I, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' are independently the same or different and each represent hydrogen, hydroxy, or lower alkoxy, or any vicinal two of R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' combined together represent --O--(CH.sub.2).sub.n --O--, wherein n=1 or 2; R.sub.4 represents methylene or halomethyl; and X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are independently the same or different and each represent hydrogen or halogen; or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition that contains an effective amount of a compound of formula I together with a pharmaceutically acceptable excipient, and a method of treating cancer that involves the administration of an effective amount of the compound of formula I to a patient in need thereof.

.alpha.-methylene peperomins and halogenated derivatives thereof

A series of novel polyamine-linked acridine dimers and derivatives thereof are described. The polyamine-linked acridine dimers and derivatives are potential anti-cancer agents.

Polyamine-linked acridine dimers

A process of preparing 2-cyano-3,5-dimethyl-4-methoxypyridine. The process includes the steps of: acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-carboxamido-3,5-dimethyl-4(1H)-pyridone; methylating 2-carboxamido-3,5-dimethyl-4(1H)-pyridone to obtain 2-carboxamido-3,5-dimethyl-4-methoxypyridine; and dehydrating said 2-carboxamido-3,5-dimethyl-4-methoxypyridone to obtain 2-cyano-3,5-dimethyl-4-methoxypyridine.

Process for preparing 2-cyano-3,5-dimethyl-4-methoxypyridine

A process of preparing 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine including the steps of acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone; halogenating 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone to obtain 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine; methoxylating 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine to obtain 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine; and reducing 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine to obtain 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine.

Process of preparing 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine

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Shan-Yen Chou