Improved Process for Ranolazine: An Antianginal Agent

被引：9

作者：

Aalla, Sampath ^{[2
]}

Gilla, Goverdhan ^{[2
]}

Anumula, Raghupathi Reddy ^{[2
]}

Kurella, Srinivas ^{[2
]}

Padi, Pratap Reddy ^{[3
]}

Vummenthala, Prabhakar Reddy ^{[1
]}

机构：

[1] Osmania Univ, Dept Chem, Univ Coll Sci, Hyderabad 500007, Andhra Pradesh, India

[2] Dr Reddys Labs Ltd, Res & Dev, Integrated Prod Dev, Ranga Reddy 500072, Andhra Pradesh, India

[3] Macleods Pharmaceut Ltd, Res & Dev, Bombay 400093, Maharashtra, India

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2012年 / 16卷 / 05期

关键词：

D O I：

10.1021/op300026r

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

An improved process has been developed for the active pharmaceutical ingredient, ranolazine with 99.9% purity and 47% overall yield (including three chemical reactions and one recrystallization). Formation and control of all the possible impurities is described. All the solvents used in the process were recovered and reused. The unreacted piperazine is recovered as piperazine monophosphate monohydrate salt.

引用

页码：748 / 754

页数：7

共 15 条

[1] THE EFFECTS OF THE NOVEL ANTI-ANGINAL COMPOUND RS43285 ON MYOCARDIAL CONDUCTION IN THE ANESTHETIZED DOG [J].

ALLELY, MC ;

ALPS, BJ .

BRITISH JOURNAL OF PHARMACOLOGY, 1988, 93 (02) :375-382

[2]

Arthur F. K., 1986, US Pat, Patent No. [4,567,264, 4567264]

[3]

Eva A.-C., 1992, [No title captured], Patent No. [0,483,932 A1, 0483932]

[4] ALPHA-(N-PIPERAZINO)DIMETHYLACETANILIDES AND THEIR LOCAL ANESTHETIC ACTIVITY [J].

FOYE, WO ;

LEVINE, HB ;

MCKENZIE, WL .

JOURNAL OF MEDICINAL CHEMISTRY, 1966, 9 (01) :61-&

[5] Ranolazine decreases diastolic calcium accumulation caused by ATX-II or ischemia in rat hearts [J].

Fraser, Heather ;

Belardinelli, Luiz ;

Wang, Lianguo ;

Light, Peter E. ;

McVeigh, Jeffrey J. ;

Clanachan, Alexander S. .

JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY, 2006, 41 (06) :1031-1038

[6] Synthesis of T2288: From bench synthesis to pilot production [J].

Guillaume, M ;

Cuypers, J ;

Vervest, I ;

De Smaele, D ;

Leurs, S .

ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2003, 7 (06) :939-941

[7] Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit [J].

Hale, Sharon L. ;

Kloner, Robert A. .

JOURNAL OF CARDIOVASCULAR PHARMACOLOGY AND THERAPEUTICS, 2006, 11 (04) :249-255

[8]

ICH, ICH HARM TRIP GUID I, pQ3C

[9] Clinical pharmacokinetics of ranolazine [J].

Jerling, M .

CLINICAL PHARMACOKINETICS, 2006, 45 (05) :469-491

[10]

Kluge A.F., 1987, [No title captured], Patent No. [EP 0,126,449, 0126449]

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