Alkylation Of An Acyclic Or Alicyclic Carbon, Which Is Adjacent To A Benzene Ring Or An Atom Double Or Triple Bonded To A Non-carbon Atom, By Means Of An Alkyl Halide, Alkyl Sulfate, Substituted Alkyl Halide Or Substituted Alkyl Sulfate Patents (Class 558/369)
  • Publication number: 20140336403
    Abstract: A process for the preparation of a compound of formula (I): which is useful as an intermediate in the preparation of pharmaceutically active compounds.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Gerard John Harnett, John Hayes, Reinhard Reents, Dennis A. Smith, Andrew Walsh
  • Publication number: 20120149895
    Abstract: The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents.
    Type: Application
    Filed: March 30, 2010
    Publication date: June 14, 2012
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Branko Jenko, Anton Copar
  • Publication number: 20120071683
    Abstract: A process for the preparation of a compound of formula (I): which is useful as an intermediate in the preparation of pharmaceutically active compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 22, 2012
    Inventors: Gerard John Harnett, John Hayes, Reinhard Reents, Dennis A. Smith, Andrew Walsh
  • Publication number: 20110009648
    Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.
    Type: Application
    Filed: January 22, 2007
    Publication date: January 13, 2011
    Applicant: Sandoz AG
    Inventors: Martin Albert, Hubert Sturm, Andreas Berger, Peter Kremminger
  • Patent number: 6774243
    Abstract: Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.
    Type: Grant
    Filed: October 30, 2001
    Date of Patent: August 10, 2004
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Qingping Tian, Naresh K. Nayyar, Srinivasan Babu, Junhua Tao, Terence Jarold Moran, Raymond Dagnino, Jr., Lennert J. Mitchell, Jr., Travis Paul Remarchuk, Michael Joseph Melnick, Steven Lee Bender
  • Publication number: 20040106818
    Abstract: A reaction of a para-substituted aryl composition with cyclohexanone is facilitated by a metal hydride, such as NaH, KH, LiH, MgH2, CaH2, AlH3, and/or LiAlH4 to make first intermediates useful in producing a drug commonly known as Venlafaxine. Alternatively, lithium diisopropylamide (diisopropylamino lithium) may be used in place of the metal hydride. The first intermediates may be further reacted to form second intermediates in a reduction that is facilitated by Rainey nickel or a metal hydride. These reaction processes may each occur in an organic solvent, which delivers highly pure reaction products in high yield.
    Type: Application
    Filed: August 11, 2003
    Publication date: June 3, 2004
    Inventors: Lan Zhiyin, Shi Kaiyun, Mo Qizhuang, Li Yulin
  • Patent number: 6215035
    Abstract: The invention relates to a process for the preparation of aralkylated aromatic compound with both small and large size aralkylating agents; wherein the catalyst used is heterogeneous solid catalyst removable from the reaction products by simple filtration, thus allowing the separated catalyst to be reused in the process. The catalyst is selected from micro or mesoporous gallosilicates and galloaluminosilicates, having structure similar to that of zeolites known in the prior art.
    Type: Grant
    Filed: January 11, 1999
    Date of Patent: April 10, 2001
    Assignee: Council of Scientific and Industrial Research
    Inventors: Vasant Ramchandra Choudhary, Suman Kumar Jana, B-Phani Kiran
  • Patent number: 5512680
    Abstract: A process is described for the preparation of (+)-2-(3,4-dichlorophenyl)-4-hydroxybutylamine (I) by reaction of 3,4-dichlorophenylacetonitrile (II) with an alkali metal halogenoacetate, treatment of the 3-cyano-3-(3,4-dichlorophenyl)propionic acid (III) with D-(-)-N-methylglucamine, with second-order asymmetric conversion, hydrolysis of the D-(-)-N-methylglucamine salt of (-)-3-cyano-3-(3,4-dichlorophenyl)propionic acid and enantioconservative reduction of the resulting levorotatory cyanoacid with a borane.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: April 30, 1996
    Assignee: Sanofi
    Inventors: Marcel Descamps, Joel Radisson, Gilles Anne-Archard
  • Patent number: 5108654
    Abstract: A method and apparatus for conducting chemical reactions in polyphase systems by using emulsifying means for the liquid components consisting of ultrasound emitters or turbines, in the absence or presence of a solid catalyst in fixed bed form with which the emulsified liquid components are brought into immediate contact by continuous circulation.
    Type: Grant
    Filed: November 17, 1988
    Date of Patent: April 28, 1992
    Inventor: Vittorio Ragaini
  • Patent number: 4760158
    Abstract: Novel 3-halo-2,2-disubstituted propanenitriles of formula ##STR1## wherein Z represents bromo or chloro and A, together with the carbon atom to which it is attached, represents a 5,6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as intermediates for preparing substituted pyrimido[1,2-a]indoles. The intermediates can be prepared by a novel process which comprises condensing a 2,2-disubstituted ethanenitrile with a dihalomethane in the presence of a non-nucleophilic strong base.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: July 26, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Ian A. Cliffe, Richard S. Todd