Organic Chemistry of Drug Synthesis. Volume 7
peptide incretin, which stimulates release of insulin by cleaving the molecule to an inactive form. Inhibition of DPP in effect ...
the product with butyllithium generates an anion on carbon next to nitro- gen. Treatment of this compound with triethyl borate d ...
establishment of the chiral locus that will dictate the remaining asymmetric centers. Oxazolidone ( 20 ), derived from valine se ...
reaction. Thus, reaction of the intermediate with carbon tetrabromide and triphenyl phosphine presumably converts the alcohol to ...
aluminum chloride yields the chloroketone ( 42 ). Reaction of that with pyrrolidine ( 40 ) leads to the alkylation product 43. C ...
attention as potential drugs. The complex fermentation product Staurosprin is a PKC inhibitor that has shown antineoplastic acti ...
Base-catalyzed Claisen condensation forms the desired six-membered ring. Heating that intermediate with base leads to saponifica ...
S F F Br+ S BuLi (Ph 3 P) 4 .Pd (^5556) NBS S F 57 Br OH (Ph 3 P) 4 .P, PPH 3 , CuI S F 58 OH HN O CO 2 C 6 H 5 Ph 3 P, DEAD S F ...
intermediate ( 65 ). Construction of the heterocyclic ring involves reaction of 65 with ammonium acetate. The reaction can be vi ...
O 68 NH 2 OH N 69 OH BuLi Ac 2 O N 70 O O CH 3 O N HO CH^3 O N CH 3 O N CH 3 ClSO 3 H 2. NH 3 71 73 72 H 2 NO 2 S Ac 2 O O 2. ...
B. Imidazoles and a Pyrrazole By now, it is well established that “conazole” antifungal agents attack fungi by inhibiting the sy ...
N (C 6 H 5 ) 3 C N CO 2 H (C 6 H 5 ) 3 C (C 6 H 5 ) 3 C (C 6 H 5 ) 3 C (C 6 H 5 ) 3 C N N H N N CH=O H N N CF 3 SO 2 H N N BuLI ...
envisaged as proceeding thorough the aminal ( 95 ) of the glyoxal. Imine formation with dichloro reagent 94 by displacement of h ...
epinephrine. Direct antagonism of the enzyme shuts down production of that neurotransmitter. This achieves an effect on the card ...
a consequence been focused on finding inhibitors of that enzyme. The first step in the convergent synthesis starts by protection ...
caused by the presence of the preexisting adjacent chiral center. The free car- boxylic acid is condensed with piperidine to for ...
HO CH=O + S NH NH O S NH NH O NaOAc AcOH HO 141 142 143 Uric acid comprises one of the principal products from metabolism of end ...
( 148 ) affords the acyl bromide. The product is then converted to the ester ( 149 ), by treatment with methanol in the presence ...
make up polysaccharide can be viewed as acetals of aldehydes. These func- tions on endogenous peptides and saccharides do occasi ...
to an aldehyde ( 160 ) by means of manganese dioxide. Aldol-type conden- sation of 160 with the active methylene group in thiazo ...
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