Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 4- and 6-position of the triazine ring, at the 1′-6′position of the ribose ring, or combinations thereof. Methods of synthesizing and manufacturing these analogs and derivatives are also provided. These compounds can be formulated into pharmaceutical compositions that can be used for treating any disease that is sensitive to the treatment with decitabine or azacitidine, such as hematological disorders and cancer.
Upon the chlorination of vinyl compounds in alcohols, the reaction products were composed of 2-alkoxy-1-chloro compound (A), 1-alkoxy-2-chloro compound (B) and vicinaldichloride (C). Various vinyl compounds were chlorinated in alcohols at 40 °C in order to elucidate the effect of their molecular structure on the product distribution. The A/(A+B) was inversely proportional to the relative rate of ordinary
[EN] PROCESS FOR THE PREPARATION OF (S)-4-METHYL-N-((S)-1-(((S)-4-METHYL-1-((R)-2-METHYLOXIRAN-2-YL)-1-OXO PENTAN-2-YL) AMINO)-1-OXO-3-PHENYLPROPAN-2-YL)-2-((S)-2-(2-MORPHOLINOACETAMIDO)-4-PHENYLBUTANAMIDO) PENTANAMIDE<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION DE (S)-4-MÉTHYL-N- ((S)-1-(((S)-4-MÉTHYL-1-((R)-2-MÉTHYLOXIRAN-2-YL)-1-OXO-PENTAN-2-YL)AMINO)-1-OXO-3-PHÉNYLPROPAN-2-YL)-2-((S)-2-(2-MORPHOLINOACÉTAMIDO)-4-PHÉNYLBUTANAMIDO) PENTANAMIDE
申请人:BIOPHORE INDIA PHARMACEUTICALS PVT LTD
公开号:WO2016046843A1
公开(公告)日:2016-03-31
Novel methods for preparation of Carfilzomib and intermediates thereof with high stereo selection are reported. The synthetic procedures result in substantially pure Carfilzomib (I).
Process for the Preparation of (S)-4-Methyl-N-((S)-1-(((S)-4-Methyl-1-((R)-2-Methyloxiran-2-YL)-1-OXO Pentan-2-YL) Amino)-1-OXO-3-Phenylpropan-2-YL)-2-((S)-2-(2-Morpholinoacetamido)-4-Phenylbutanamido) Pentanamide
申请人:Biophore India Pharmaceuticals Pvt. Ltd
公开号:US20170298093A1
公开(公告)日:2017-10-19
Novel methods for preparation of Carfilzomib and intermediates thereof with high stereo selection are reported. The synthetic procedures result in substantially pure Carfilzomib (I).
Processes for the preparation of biotinylated polynucleotides and analogues thereof and protected intermediate products for use in such processes are described and claimed. The processes may be conveniently used in the automated synthesis of biotinylated polynucleotide on a DNA synthesiser. The polynucleotides so prepared may be used as labelled probes e.g. as diagnostic tools for clinical and research uses.
本发明描述并声称了制备生物素化多核苷酸及其类似物的工艺以及用于此类工艺的受保护中间产物。这些工艺可方便地用于在 DNA 合成器上自动合成生物素化多核苷酸。这样制备的多核苷酸可用作标记探针,如临床和研究用的诊断工具。