TAILIEUCHUNG - Pharmaceutical Substances Syntheses, Patents, Applications - Part 1

Pharmaceutical Substances Syntheses, Patents, Applications - Part 1. Reference containing a collection of 2267 active pharmaceutical ingredients, including those launched recently. Listed alphabetically according to their INNs and established a link between INNs, structure, synthesis and production processes, patent and literature situation, medical use, and trade names. For pharmacists and researchers | Abacavir A 1 Abacavir 1592U89 ATC J05AF06 Use antiviral anti HIV reverse transcriptase inhibitor RN 136470-78-5 MF CI4H18N6O MW CN 1 S 4R -4- 2-Amino-6- cyclopropylamino -97ï-purin-9-yl -2-cyclopentene-1 -methanol succinate RN 168146-84-7 MF C14HI8N6O C4H6O MW sulfate RN 188062-50-2 MF C14H18N6O 1 2H2SO4 MW 0 h3c h3C poci3 n c2h5 3 ---------------- I guanidine diethyl malonote 2-amina-4 6- pyrimidinedione 2-amino-6-chloro-4 3H -pyrimidinone I 1. hno3 0 0 2. h3c- x h3 0 0 HN N02 1. P0CI3 2. H2 Pd-C B Cl H C N 3 H 2-acetylamino-6-chloro-5-nitro-4 3H -pyrimidinone Cl 0 N-VH2 JI H zi H C N N Cl 3 H N- 5-amino-4 6-dichloropyrimidin-2-yl acetomtde 11 HCOOH CH3CO 2O ------------- formic acid Cl H 0 CH0 3 H . N- 4 6-dichloro-5- formylamino -2-pyri- midinyt acetamide HI n c2h5 3 c2h5oh -------------------- 1S-cis -4-amino-2-cyclopentene-1-methanol IV VII acetic ocid diethoxymethyl ester VI t 2 A Abacavir vu cyclopropyl-omine VIH oa synthesis of lS-cis -4-amino-2 cyclopentene-1-methanol IV NCO cyclo- 4-methylbenzene pentadiene sulfonyl isocyanate 2- azabicycto- hept-5-en- 3- one DC ß-lactamase pH 7 enzymatic stereoselective hydrolysis --------------------------------------- h2N COOH LiAIH4 --------- IV cis-4-amino-2-cyclopentene-1 -carboxylic acid 0 4 S -benzyl- 4-pentenoic pivalic X oxazolidin-2-one anhydride Bu2B0T --------------- dibutyl boryl tritiate acrolein QÇI f C6H 3 Ph-CH Ru-CI I 2 ch2ci2 p c6h 3 ----------------------- Grubb s catalyst LiBH4 THF CH-jOH -------------- 5 R - hydroxy-methyl -2-cyclopenten-1 R -oI XII XI Abacavir A 3 XII H3C Y 3 0 methyl chloroformate TEA DMAP CH2CI2 --------------------- xni NaH THF DMSO xm Cl Pd PPh3 4 _VII VIII ------- Abocavir tetrakis triphenyl- phosphine pallodium 2-omino-6- chloropurine cf. famciclovir roc-IV TEA 1 -butanal --------------- 2-amino-4 6-dichloropyrimidine -cis-4- 2-amina-4- chloro-6-pyrimrdinyl - amina -2-cyclopentene- 1-methanol XIV XIV 1. Ac-ONa CH3COOH 2. Zn CHjCOOH

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