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  • Process For Dexmethylphenidate

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    sunil_vaman_joshi
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    Process for preparation of Dexmethylphenidate

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    Process for Dexmethylphenidate

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    Process for preparation of Dexmethylphenidate

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    12 tayangan5 halaman

    Process For Dexmethylphenidate

    Diunggah oleh

    sunil_vaman_joshi
    Process for preparation of Dexmethylphenidate

    Hak Cipta:

    © All Rights Reserved
    Unduh sebagai PDF atau baca online dari Scribd
    Tandai sebagai konten tidak pantas
    dari 5
    2 United States Patent Gupte et al. ‘US010081597B2 US 10,081,597 B2 Sep. 25, 2018 (a0) Patent No. 4s) Date of Patent: (54) PROCESS FOR PREPARATION OF DEXMETHYLPHENDATE, HYDROCHLORIDE (71) Applicant: Embio Limited, Mumbai (IN) (72) Inventors: Ashutosh Digambar Gupte, Mumbi (IN); Sunil Vaman Joshi, Mumbsi (IN); Amit Hari Pakhurde, Mumbai aN) oe Assignee: Emblo Limited, Mumbai (IN) (*) Notice: Subject to aay disclaimer the term ofthis patent is extended or adjusted under 35 USC. 154(b) by 0 days ey Appl. Nos 15) 20511 (22) PCT Filed: Nov. 3, 2014 (86) PCT No. $371 @XD, (2) Date PCTB20149065763 Dec. 20, 2016 (87) PCT Pub, No: Wo201s/198108 PCY Pub, Date: Dee. 30, 2015 ) Prior Publication Data US 201710217886 Al Avg. 3, 2017 G0) Foreign Application Prlority Data Jun, 27, 2014 (IN) 2090/MUMI2014 (51) Intl cov 21034 (2) US.CL PC (2006.01) CO7D 211/34 (2013.01); C7B 220007 (2013.01) (58) Fleld of Classification Seareh Pc COTD 21134; CO7B 2200/07 uspc 546/238 See application file for complete search history. 66) References Cited US. PATENT DOCUMENTS 6.100401 4 * $2000 Prashad cov 204 546.253 6162919 4122000 Prashad 91063100 B2 62015 Nason 9.204460 2122015 Opiate 20080277791 AL 122005 Nishiyama etal FOREIGN PATENT DOCUMENTS wo swm2s902 6 1998 (OTHER PUBLICATIONS, Alivich Catalogue 1998-1999, p 10, p. 699, 3 pages * * cited by examiner Primary Examiner — Taylor V Oh (74) Auornes, Agent, or Firm —Blueshift IP, LLC Robert Plotkin on The present invention relates toa process for preparation of dexmethylpheaidate hydrochloride from racemic methyl phenidate. The process involves the treatment of racemic nixture of d-threo-methy|phenidate base in the presence of ipivaloy!-D-tararie acid (D-DPTA) in a solvent to isolate ipivaloyl tartrate salt of d-threo-methyphenidate. The ipivaloyltanrate salt of d-threo-methyiphenidat is treated witha base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent, The ¢-threo-methy phenidate base is treated with hydrochloric aci-isopropy! ‘aleohol solution to obtain slur of d-threo-methylphenidate hydrochloride also known as’ dexmethylphenidate hydro chloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone, The invention also dis closes a process for recovery of D-DPTA from the salt ‘mother liquor and from the spent aqueous layer. The process {is economical, environmental iendly and results in increased yield and optically pure dexmethylphenidate hydrochloride, ABSTRACT 10 Claims, No Drawings ‘US 10,081,597 B2 1 PROCESS FOR PREPARATION OF DEXMETHYLPHENIDATE HYDROCHLORIDE ‘TECHNICAL FIELD OF THE INVENTION ‘The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic meth- ylphenidate. The process involves the preparation of tartaric salts of methylphenidate and conversion of tartaric salts of methylphenidate to enantiomers of methylphenidate hydro- chloride, BACKGROUND OF THE INVENTION Methylphenidate hydrochloride is « psychostimulant of phenethylamine class. The dmug is safe, effective and ‘approved forthe treatment of atention-dficit hyperactivity disorder (ADHD), postural orthostatic tachycardia. syn- ‘drome and narcolepsy in human, Long-term teatment with, methyiphenidate hydrochloride ineeases the activity of en teal nervous system, reduces the structural and functional slbnommalites in the brain, Dexmethylphenidate, also known a8 d-threo-methyl- phenidate(D-TMP) isa dextortstory enantiomer of meth- 2 Yinhenidat, which is also effective psychostimulant against ADHD. Dexmethyiphenidate is the (RR) enantiomer of inetyiphenidae ‘Racemic methylphenidate contains both dexto- and Levo- rotatory methyphenidate which ae wsefl forthe treatment ‘ofADHD. Iis very challenging to isolate a puritid form of

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