Light Sciences Oncology Inc.

Purdue Pharmaceutical Products L.p.

Leon Xu

Alexander J Pallenberg

An improved two stage reaction process for production of mono-L-aspartyl chlorin e. In a first stage, the activation reaction between chlorin eand a carbodiimide produces a previously unknown anhydride in an activation reaction product (Formula I). This reaction product is purified to remove a significant proportion of the precursors of di-L-aspartyl chlorin e. The purified activation reaction product contains a higher concentration of the previously unknown anhydride. This purified reaction product is used in a second stage: a coupling reaction of the purified activation reaction product with aspartate. The coupling reaction produces a coupling reaction product that has significantly reduced di-L-aspartyl chlorin e6 concentration. This reduced di-L-aspartyl chlorin e6 concentration facilitates purification of mono-L-aspartyl chlorin e6 from the coupling reaction mixture. 

Compositions and methods of making a photoactive agent

A composition of matter of an anhydride of formula 1 below and an improved two stage reaction process for production of mono-L-aspartyl chlorin e, utilizing the anhydride: 

An improved two stage reaction process for production of mono-L-aspartyl chlorin e. In a first stage, the activation reaction between chlorin eand a carbodiimide produces a previously unknown anhydride in an activation reaction product. This reaction product is purified to remove a significant proportion of the precursors of di-L-aspartyl chlorin e. The purified activation reaction product contains a higher concentration of the previously unknown anhydride. This purified reaction product is used in a second stage: a coupling reaction of the purified activation reaction product with aspartate. The coupling reaction produces a coupling reaction product that has significantly reduced di-L-aspartyl chlorin e6 concentration. This reduced di-L-aspartyl chlorin e6 concentration facilitates purification of mono-L-aspartyl chlorin e6 from the coupling reaction mixture.

Growing community of inventors

Issaquah, WA, United States of America

Leon Xu