Abstract:
A method for producing a β-enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula (I); and b) quenching the reaction mixture of step a) with a base. The β-enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.
Abstract:
A method for screening cells with high level expression of a target protein is disclosed. The method includes introducing into a plurality of host cells a DNA construct that encodes both a target protein and an inhibitor to an endogenous selectable marker in the host cells, screening host cells harboring the DNA construct for the expression of the endogenous selectable marker, and isolating cells with reduced expression of the selectable marker. Also disclosed is a DNA construct configured to express both the target protein and the inhibitor inside the host cell.
Abstract:
The present invention provides a novel semi-synthetic method of producing a variety of novel taxane derivatives. The method involves the reaction of a phenylisoserine derivative with a suitably blocked Baccatin III derivative to produce a taxane substrate that may be further modified to form Pactitaxel and other potentially useful taxane derivatives.
Abstract:
[00110] The present application provides intermediates for preparing prostaglandin analogues and processes for preparing prostaglandin analogues and intermediates thereof. The intermediates include: A compound of formula (6) Ri represents H, C 1 -C 5 -alkyl, or benzyl, in particular isopropyl.
Abstract:
New crystalline polymorph of exemestane characterized by a powder X-ray diffraction pattern having peaks at 10.7±0.1, 15.9±0.1, and 18.1 ±0.1 2- theta degree.
Abstract:
The key intermediate in any synthesis of Irinotecan is 7-ethyl-10-hydroxy-20(S) camptothecin. A process for the efficient synthesis of this intermediate is demonstrated proceeding through readily availabe 20(S)-camptothecin. Various other tecan compounds may be made by use of corresponding 7-alkyl-10-hydroxy-20(S)-camptothecin intermediates.
Abstract:
The present invention provides an efficient synthetic process for making benazepril and analogues thereof by having an intermediate compound undergo epimerization and kinetic resolution.