TAILIEUCHUNG - Pharmaceutical Substances Syntheses, Patents, Applications - Part 70

Pharmaceutical Substances Syntheses, Patents, Applications - Part 70. 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 | Docetaxel D 691 Troc-CI pyridine ci 10-deocetylboccotin UI extracted and purified from leaves of Toxus baccato L. Troc x O CCIj 0 DCC DMAP toluene ----------------k 4-dimethylomino-pyridine threo-2- 1-ethoxyeth-oxy -3- tert-butoxy-corbonylomino -3-phenylpropîonic ocid II an Q H- C Ll Boc Û 3 Vch3 O CH _CH3 O-x CH3 aa synthesis of intermediate 1. NaN3 C2H5OH 2. HCI C2H5OH 3. H2 Pd-C C2H5OH 1. sodium azide tert-butyl 3-phenylglycidate ethyl threo-3-omino-2-hydroxy-3-phenyl-propionate IV 692 D Docetaxel IV 1. Boc o Boc V . ch2ci2 2. H2CiXO CH3 . CH2CI2 H 3. LiOH C2H6OH -------------------------- 1. di-tert-butyl dicorbonote 2. vinyl ethyl ether n e electrochem. reduction CHjCOOH NoOAc. CH3OH III ------------------------- Docetoxel N C2Hs 3 ether dibutylborotriflate --------------------- vn 4S 5R -3- 2-bromo- benz- acetyl -4-methyl-5- aldehyde phenyl-2-oxozolîdinone hexane THF vn ethyl 2R 3R -3-phenyl-2-oxirane-carboxylote VIII Docetaxel D 693 1. NoNj Jpi5OH 2. H2 Pd-C ethyl acetate 3. V CH2CI2 ethyl 2R 3S -3-tert-butaxy-carbonylamino-2-hydroxy-3-phenylpropîonate IX 1. TosOH pyridine toluene CH3 2- LiOH C- H5OH 2-methoxy- propene Boc-N O HjŒCHj 4S 5R -3-tert-butoxy-carbonyl-2 2-dimethyl-4-phenyl-5-oxazolidine-carboxylic acid X da alternative synthesis of intermediate X CH OH Pi 1 2-v O Y M 1 Boc. 1 n HoN COOH N Y XCH L H 0 S -phenylglycine XII 1. DIBAL toluene 2- P tetrabutyl ammonium fluoride 1. dibutylalumînum hydride 2. 2- trimethylsily1 thiozole tert-butyl 1S 2R -2-hy-draxy-1 -phenyl-2- 2-thia-zolyl ethylcarbamate XIII

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