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1. (WO2017157352) A PREPARATION METHOD OF DIASTEREOMERICALLY PURE TENOFOVIR ALAFENAMIDE OR ITS SALTS
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Pub. No.: WO/2017/157352 International Application No.: PCT/CZ2017/000009
Publication Date: 21.09.2017 International Filing Date: 20.02.2017
IPC:
C07F 9/6561 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6561
containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Applicants:
ZENTIVA, K.S. [CZ/CZ]; U Kabelovny 130 102 37 Praha 10, CZ
Inventors:
STEFKO, Martin; CZ
MAN, Stanislav; CZ
Agent:
JIROTKOVA, Ivana; ROTT, RUZICKA & GUTTMANN Vinohradska 37, 120 00 Praha 2, CZ
Priority Data:
PV 2016-15617.03.2016CZ
Title (EN) A PREPARATION METHOD OF DIASTEREOMERICALLY PURE TENOFOVIR ALAFENAMIDE OR ITS SALTS
(FR) PROCÉDÉ DE PRÉPARATION DE TÉNOFOVIR ALAFÉNAMIDE DIASTÉRÉOMÉRIQUEMENT PUR OU DE SES SELS
Abstract:
(EN) The invention relates to an efficient preparation method of diastereomerically pure Tenofovir Alafenamide (TA) of structure la with the absolute configuration (S) at the phosphorus atom - Sp-diastereoisomer. Tenofovir Alafenamide Fumarate of formula 2 (TAF) is a reverse transcriptase inhibitor, which is currently in the clinical study stage as a prodrug of Tenofovir 3 for the treatment of HIV infection and hepatitis B. Compared to the hitherto used prodrug, Tenofovir disoproxil fumarate of formula 4, TAF exhibits greater antiviral activity and better distribution in the lymphatic system.
(FR) L'invention concerne un procédé efficace de préparation de ténofovir alafénamide (TA) diastéréomériquement pur de structure la ayant la configuration absolue (S) au niveau du diastéréo-isomère à atome de phosphore S p. Le fumarate de ténofovir alafénamide de formule 2 (TAF) est un inhibiteur de la transcriptase inverse, qui est actuellement à l’étape d’étude clinique en tant que promédicament du ténofovir 3 pour le traitement de l’infection à VIH et de l’hépatite B. Par rapport au promédicament utilisé jusqu’à présent, le fumarate de ténofovir disoproxil de formule 4, le TAF présente une activité antivirale plus élevée et une meilleure distribution dans le système lymphatique.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)