发明名称 |
AN IMPROVED PROCESS FOR THE PREPARATION OF PURE PALONOSETRON HYDROCHLORIDE |
摘要 |
<p>The present invention relates to an improved and industrially viable process for the preparation of high purity >99.8% chemical and >99.8% chiral of palonosetron hydrochloride of formula-I ((3as)-2[(3s)-1-azabicyclo [2.2.2] oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinoline-1-one monohydrochloride) obtained from reduction of 2-[(S)-1-azabicyclo[2.2.2]oct-3-yl]-2,4,5,6-tetrahydro-1H-benz[de]iso-quinolin-1-one hydrochloride of formula-VI. In the prior art compound of formula-VI or its base are used in the catalytic hydrogenation. But the selection of solvents like acetic acid or THF rendered them commercially not viable due to low yield and low purity of palonosetron hydrochloride. In the present process simple solvent like methanol and readily available palladium-on-carbon were used to increase the yield and purity of palonosetron hydrochloride. Palonosetron Hydrochloride is useful as anti-emetic agent during the chemotherapy of treatment of cancer patients and is marketed under the brand names 'Aloxi' and 'Onicit'.</p> |
申请公布号 |
WO2009010987(A1) |
申请公布日期 |
2009.01.22 |
申请号 |
WO2008IN00313 |
申请日期 |
2008.05.16 |
申请人 |
NATCO PHARMA LIMITED;RAVI, JANAKI RAMA RAO;PULLA REDDY, MUDDASANI;ADIBHATLA KALI SATYA, BHUJANGA RAO;VENKAIAH CHOWDARY, NANNAPANENI |
发明人 |
RAVI, JANAKI RAMA RAO;PULLA REDDY, MUDDASANI;ADIBHATLA KALI SATYA, BHUJANGA RAO;VENKAIAH CHOWDARY, NANNAPANENI |
分类号 |
C07D453/02;A61K31/439;A61P1/08 |
主分类号 |
C07D453/02 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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