Samsung Electronics Co., Ltd.

Min-Hwan Kim

Do-Yun Kim

Young-Hee Kim

Bong-Seok Moon

Jae-Chan Park

Seung-Joo Seo

Young-Jun Park

Ho-Seong Lee

Kyung-Chul Kim

Disclosed is a process for preparing arrays of oligopeptide nucleic acid probes immobilized on a solid matrix by employing polymeric photoacid generator. Arrays of peptide nucleic acid probes of the invention are prepared by the steps of: (i) derivatizing the surface of a solid matrix with aminoalkyloxysilane in alcohol and attaching a linker with acid-labile protecting group on the solid matrix; (ii) coating the solid matrix with polymeric photoacid generator(PAG); (iii) exposing the solid matrix thus coated to light to generate acid for eliminating acid-labile protecting group; (iv) washing the solid matrix with alkaline solution or organic solvent and removing residual polymeric photoacid generator; and, (v) attaching a monomeric peptide nucleic acid with acid-labile protecting group to the solid matrix, and repeating the previous Steps of (ii) to (v). In accordance with the present invention, neutral peptide nucleic acid probes, as the promising substitute for conventional negatively-charged oligonucleotide probes, can be prepared by employing polymeric photoacid generator in a simple and efficient manner, while overcoming the problems confronted in the prior art DNA chip fabrication using PR system and PPA system.

Process for preparing peptide nucleic acid probe using polymeric photoacid generator

The present invention relates to a process for preparing arrays of oligopeptide nucleic acid probes immobilized on a solid matrix by employing polymeric photoacid generator. Arrays of peptide nucleic acid probes of the invention are prepared by the steps of: (i) derivatizing the surface of a solid matrix with aminoalkyloxysilane in alcohol and attaching a linker with acid-labile protecting group on the solid matrix; (ii) coating the solid matrix with polymeric photoacid generator (PAG); (iii) exposing the solid matrix thus coated to light to generate acid for eliminating acid-labile protecting group; (iv) washing the solid matrix with alkaline solution or organic solvent and removing residual polymeric photoacid generator; and, (v) attaching a monomeric peptide nucleic acid with acid-labile protecting group to the solid matrix, and repeating the previous Steps of (ii) to (v). In accordance with the present invention, neutral peptide nucleic acid probes, as the promising substitute for conventional negatively-charged oligonucleotide probes, can be prepared by employing polymeric photoacid generator in a simple and efficient manner, while overcoming the problems confronted in the prior art DNA chip fabrication using PR system and PPA system.

Disclosed is a process for preparing optically active (&minus;)pyridobenzoxazine carboxylic acid derivative and pharmaceutically acceptable salt thereof by employing a starting material of (&plus;)ethyl 2-(4-chloro-5-fluoro-2-halo-3-nitobenzoyl)-3-&lsqb;(1-hydroxypropy-2(s)-yl)amino&rsqb;acrylate. According to the present invention, optically active (&minus;)pyridobenzoxazine carboxylic acid derivative can be manufactured from low-priced 4-chloro-5-fluorobenzoic acid derivative in a simple and economical manner.

Process for preparing (-)pyridobenzoxazine carboxylic acid derivatives

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Taejon, South Korea

Min-Hwan Kim