Pharmaceutical Substances Syntheses, Patents, Applications - Part 197. 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. | Tacrolimus T 1961 1. Li CHj HjC I 0 2. N-Br . benzene 0 X -------------------------- intermedióte XIX M OH HO OH OH OH L-arobinitol 0 h 04 p CHj Cl a-acetoxy-isobutyryl chloride 1. NoOCHj THF 2. Tbs Cl THF 1. sodium methoxide 2. tert-butyldimethyl-silyl chloride 1. lK - ch3 vn 2. BF3 O C2H5 2 2. boron trifluoride etherate xin XIII HgCI2 Tas-OH C2H5OH -------------------------- mercury II chloride p-toluenesulfonic acid XIV 1. Lr h3cvnvch3 THF ch3ch3 2. HF CH3CN 3. CI3CyO xO F3C-S03H NH --------------------------------- 1. lithium diisopropylamide methyl iodide 2. hydrogen fluoride in acetonitrile 3. benzyl trichloroacetimidote in trifluoromethansulfonic acid XV 1. CH3OH NoH 2. H3C-I DMF 3. H2. Pd-C 1. methanol sodium hydride 2. methyl iodide 3. hydrogen CHjO 0 CH3 ch3ch3 XVI 1962 T Tacrolimus 1. T0S-0H CH 2. Li B H û . THF -CH3 3. BF3 O C2H5 2 HS SH XVI ---------------------------------- 1. pyridinium p-taluenesulfonate 2. L-selectride 3. boron trifluoride etherate 1 3-propanedithiol XVII XVII 1. LiAlH4 1. lithium aluminum hydride 2 triphenylphosphine iodine XVIII 1. n c2h5 3 ch2ci2 2 H3Ç fl CHj N-P H C I CH 3 XH 3 0 J Lix CH3 THE xviii Tbs-0 S CF3---------------------------------- II 2. ethylphosphonic acid bis dimethylamide butyllithium tert-butyldimethyl-silyl trifluoromethonesulfonote ch3 0 px ch3o ch3ch3 -ch ch3ch3 CH3 3 XIX Tacrolimus XX 1. DCC 2. Zn NH4CI N-tert-butoxycarbo- XXI nylpiperidine-2 S - corboxylic acid Boc CH3 0- -ch3 ch3 Tacrolimus T 1963 XXI XIX 1. Lix x- CH3 2. CH3OH X O I 0 JJ K H f3c o o cf3 3. CH3C00H 1. butyllithium 2. methanol bis trifluoro acetoxy iodo benzene 3. acetic acid XXII O XXII ch3 Dmt O Li H3C N CH3 THF ch3ch3 xxni lithium diisopropylamide methyl 2- 2 4-dimethoxyben-zyloxy acetate Dmb N CH. 1- I ï 2. N-methyl-2-chloro-pyridînium iadîde n c2h5 3 ------------------- --- . XXIV 1. 2 6-dimethylpyridine xxm ------------------------------------ XXVI 1. trifluoroacetic acid in THF 2. Dess-Mortin periodinone XXV THF
