AR051302A1 - A PROCEDURE TO PREPARE SAQUINAVIR USING AN INTERMEDIARY - Google Patents

A PROCEDURE TO PREPARE SAQUINAVIR USING AN INTERMEDIARY

Info

Publication number
AR051302A1
AR051302A1 ARP050104036A ARP050104036A AR051302A1 AR 051302 A1 AR051302 A1 AR 051302A1 AR P050104036 A ARP050104036 A AR P050104036A AR P050104036 A ARP050104036 A AR P050104036A AR 051302 A1 AR051302 A1 AR 051302A1
Authority
AR
Argentina
Prior art keywords
formula
saquinavir
intermediary
prepare
procedure
Prior art date
Application number
ARP050104036A
Other languages
Spanish (es)
Inventor
Reddy Bandi Parthasaradhi
Reddy Kura Rathnakar
Reddy Rapolu Raji
Kumar Dandamudi Satish
Original Assignee
Hetero Drugs Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hetero Drugs Ltd filed Critical Hetero Drugs Ltd
Publication of AR051302A1 publication Critical patent/AR051302A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Reivindicacion 1: Un procedimiento para preparar saquinavir de la formula (1) o una sal farmacéuticamente aceptable del mismo caracterizado porque comprende. A) hacer reaccionar N2-(2-quinolinilcarbonil)-L-asparagina de la formula (2) con cloruro de pivaloilo de formula (3) en presencia de una base orgánica para obtener un anhídrido mixto de formula (4); b) hacer reaccionar el anhídrido mixto de formula (4) con [3S, 4aS, 8aS]-2-(3(s)-amino-2-( R )-hidroxi-4-fenilbutil -N-(1,1- dimetiletil)decahidro-3-isoquinolina carboxa-mida de formula (5) para obtener saquinavir de la formula (1) y opcionalmente convertir saquinavir en sus sales ácidas de adicion farmacéuticamente aceptables. Reivindicacion 13: Compuesto de formula (4).Claim 1: A process for preparing saquinavir of the formula (1) or a pharmaceutically acceptable salt thereof characterized in that it comprises. A) reacting N2- (2-quinolinylcarbonyl) -L-asparagine of the formula (2) with pivaloyl chloride of formula (3) in the presence of an organic base to obtain a mixed anhydride of formula (4); b) react the mixed anhydride of formula (4) with [3S, 4aS, 8aS] -2- (3 (s) -amino-2- (R) -hydroxy-4-phenylbutyl -N- (1,1- dimethylethyl) decahydro-3-isoquinoline carboxa-mida of formula (5) to obtain saquinavir of the formula (1) and optionally converting saquinavir into its pharmaceutically acceptable acid addition salts Claim 13: Compound of formula (4).

ARP050104036A 2005-06-16 2005-09-26 A PROCEDURE TO PREPARE SAQUINAVIR USING AN INTERMEDIARY AR051302A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IN2005/000204 WO2006134612A1 (en) 2005-06-16 2005-06-16 A process for the preparation of saquinavir using novel intermediate

Publications (1)

Publication Number Publication Date
AR051302A1 true AR051302A1 (en) 2007-01-03

Family

ID=37531996

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050104036A AR051302A1 (en) 2005-06-16 2005-09-26 A PROCEDURE TO PREPARE SAQUINAVIR USING AN INTERMEDIARY

Country Status (2)

Country Link
AR (1) AR051302A1 (en)
WO (1) WO2006134612A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120035211A1 (en) * 2009-02-17 2012-02-09 Hetero Research Foundation Novel polymorphs of saquinavir
CN102260243B (en) * 2011-06-09 2013-08-14 沈阳亿灵医药科技有限公司 Saquinavir succinic acid half ester salt and its preparation
CN111013309B (en) * 2019-12-17 2022-01-14 南通市天时化工有限公司 Method for purifying tail gas and recovering materials in pivaloyl chloride production process

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8927913D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives

Also Published As

Publication number Publication date
WO2006134612A1 (en) 2006-12-21

Similar Documents

Publication Publication Date Title
CY1108101T1 (en) PYRIMIDINE COMPOUNDS AND THEIR USE IN PREPARING A TRIZOLO-PYRIMIDINE NUCLEOZITE
EA200702589A1 (en) 2,6-quinoline derivatives, methods of their production and their use
EA200700387A1 (en) HYDRATES AND POLYMORPHES 4 - [[(7R) -8-CYCLOPENTYL-7-ETHYL-5,6,7,8-TETRAHYDRO-5-METHYL-6-OXO-2-PTERIDINYL] AMINO] -3-METHOXY-N- (1-METHYL-4-PIPERIDINYL) BENZAMIDE, METHODS OF THEIR PRODUCTION AND THEIR APPLICATION AS A MEDICINE
DK1791571T3 (en) Radiofluorinated peptides
TW200640913A (en) 5-Substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents
CY1112738T1 (en) A COMBINED COMPOSITION CONTAINING Ibuprofen And Paracetamol
CY1112019T1 (en) NIACINI RECEPTORS RACE, COMPOSITIONS CONTAINING COMPOSITIONAL COMPOUNDS AND METHODS OF TREATMENT
ATE401875T1 (en) PHARMACEUTICAL SOLID DISPERSIONS OF MODAFINIL COMPOUNDS
UA88481C2 (en) Donepezil fumarate suitable for the preparation of pharmaceutical compositions
PE20110677A1 (en) N- (2-AMINOPHENIL) -4- [N- (PYRIDIN-3-IL) METOXYCARBONYLAMINE-METHYL] BENZAMIDE (MS-275) POLYMORPH B
ATE424821T1 (en) PYRROLOPYRIDINE-2-CARBONIC ACID AMIDES
RS52108B (en) 3-substituted-[1,2,3]-benzotriazinone compound for enhancing glutamatergic synaptic responses
ES2541857T3 (en) Processes for preparing cyclopropylamides and intermediates associated with these
ECSP11011286A (en) SOLID ORAL FORMULATIONS OF A PYRIDOID-PYRIMIDINONE
AR051302A1 (en) A PROCEDURE TO PREPARE SAQUINAVIR USING AN INTERMEDIARY
MY138698A (en) Method for synthesis of (2s)-indoline-2-carboxylic acid, and use in the synthesis of perindopril
EA200701962A1 (en) ADDITIVE SALT TOLPERIZON, METHOD OF THEIR RECEPTION AND THEIR APPLICATION
EA201301136A3 (en) NEW METHOD OF SYNTHESIS (2E) -3- (3,4-DIMETOXYPHENYL) PROP-2-ENNITRIL, APPLICATION IN IVABRADINE AND ITS PHARMACEUTICAL ACCEPTIVE SALTS
ATE405588T1 (en) ANALOGUES OF SOMATOSTATIN
EP1872780A3 (en) Omega-Phenyloctanamides as therapeutic compounds
MY142634A (en) Method for synthesis of (2s,3as,7as)-perhydroindole-2-carboxylic acid and esters thereof, and use in the synthesis of perindopril
RU2008105610A (en) METHODS FOR PRODUCING N-Acyl DERIVATIVES OF AMINO ACIDS (OPTIONS)
ZA200706707B (en) 1H-indole-3-carboxylic acid derivatives and their use as PPAR agonists
TW200640868A (en) 5-Substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents
Chen et al. Stereoselective Synthesis of 2, 3, 4, 5-Tetrasubstituted trans-2, 3-Dihydrofuran Derivatives

Legal Events

Date Code Title Description
FB Suspension of granting procedure