Development Center for Biotechnology

Development Center of Biotechnology

Shyh-Fong Chen

Shan-Yen Chou

Hao Ku

Shan-Shue Wang

Wen-Chih Chou

Tsai-Mien Huang

Ming-Chen Chou

Hsiu-Chih Yeh

Chin-Fen Lee

Fan-Jung Liu

Pao-Nien Chen

Shu-Chien Liu

Hsiang-Ling Huang

Pao-Chiung Hong

Yann-Yu Lu

Ohm-Guo Pan

Adam Shih-Yuan Lee

Han-Jung Tsai

Hou Ku

Lee Tai Liu

Wei-Kun Yin

Chang-Wei Tan

An aqueous inhalation pharmaceutical composition comprising a polypeptide or protein is provided. The composition of the present invention can improve the bioavailability of the polypeptide and protein, and avoid inducing toxicity in the lung.

Aqueous inhalation pharmaceutical composition

A new method for the preparation of chiral 4-substituted 2-piperidinones, trans-3,4-disubstituted 2-piperidinones, and trans-3,4-disubstituted piperidines is invented. Chiral paroxetine can be obtained from a chiral trans-3,4-disubstituted piperidine intermediate in high purity and good selectivity.

Practical syntheses of chiral trans-3, 4-disubstituted piperidines and the intermediates

The present invention relates to a process for the preparation of amides, comprising reacting amines with carboxylic acids in the presence of silicon amines. The present invention further relates to a process for the preparation of quinazoline derivatives, comprising reacting amines with carboxylic acids in the presence of silicon amines to obtain amides and contacting the resultant amides with quinazoline.

Preparation of amides and quinazoline derivatives

The present invention provides a process for preparing an amide, which comprises reacting an amine with an ester in a molten form in the absence of a solvent.

Process for preparing amides

A process for preparing optically active allylic alcohol derivatives comprises reacting a racemic mixture of the following formula I ##STR1## wherein R is alkyl, alkenyl, or substituted or unsubstituted aryl or arylalkyl; with acetate or anhydride under the catalysis of Pseudomonase AK, PS or K-10 lipase in the presence of an organic solvent.

Process for preparing optically active allylic alcohol 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.

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Taipei, Taiwan

Shyh-Fong Chen