Organic Chemistry of Drug Synthesis. Volume 7
of methyl 4-methylacetoacetate ( 73 ) withp-fluorobenzaldehyde to afford the acrylate ( 74 ). This last intermediate is then rea ...
(C 6 H 5 )P CO 2 CH 3 O OSiMe(CH 3 ) 2 tBu OSiMe(CH^3 )^2 tBu N F N N SO 2 CH 3 79 + N F N N SO 2 CH 3 81 CH 3 80 CH=O O CO 2 CH ...
CH 3 OC O OCH 3 (CH 3 ) 3 Si Si(CH 3 ) 3 Cl O (CH 3 ) 3 Si O NaBH (^4) (CH 3 ) 3 Si OH AlCl 3 CH 3 O 2 C OH CH 3 O OCH 3 CH 2 C ...
An entire new field of therapeutics arose with the serendipitous discovery of the effect of sildefanil, far better known as Viag ...
sequence, 5-FU is first converted to the silylated derivative ( 109 ) by means of trimethylsilyl chloride. Treatment of that wit ...
HO H O O 117 C 2 H 5 O H 3 C O 118 H 2 N NH 2 S 119 + SbCl 3 HO NH NH H 3 C S C 2 H 5 O O 120 Half of the bases in RNA and DNA c ...
The preparation of this agent starts with the fully protected arabinose derivative ( 121 ). Treatment of 121 with hydrogen bromi ...
by tributyl tin ( 135 ). Treatment of 135 with potassium fluoride results in cleavage of the silicon–oxygen bonds, as well as re ...
142 with the silylated derivative 144 in the presence of Lewis acid leads to the coupling product 145 with loss of the silyl gro ...
with 2-chloropyrimidine ( 157 ) to afford 158. Yet another hydrogenation reduces the heterocyclic ring to a tetrahydropyrimidine ...
O tBuO 2 C +H^2 N BO tBuO 2 C NH CO 2 H 160 161 NH O HN BO O N N O HN BO O N N NH O 162 164 IBuB(OH) 2 OH HN B OH O N N NH O 165 ...
by reaction of the thus-formed amine withtert-butyloxycarbonic anhydride leads to intermediate 170 as a single diastereomers.^25 ...
Reductive amination of 177 via the aldehyde group in the phenoxy acid 178 affords 179.^26 At least several weeks administration ...
D.W. Ludovici et al.,Bioorg. Med. Chem. Lett. 11 , 2235 (2001). M. Ubasawa, S. Yuasa, U.S. Patent 5,604,209 (1997). M. Watanabe ...
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CHAPTER 7 FIVE-MEMBERED HETEROCYCLES FUSED TO ONE BENZENE RING 1. COMPOUNDS WITH ONE HETEROATOM A. Benzofurans The presence of t ...
presence of mild base would then lead to the antiarrythmic agent dronedar- one ( 9 ).^1 O 2 N OH 1 PPh 3 O^2 NO^2 N O 2 N OH 2 O ...
O HO O 10 + F MgBr 11 OH O HO F 12 O O HO F OtBu O 13 Br N(CH 3 ) 3 N(CH 3 ) 3 N(CH 3 ) 3 O OH HO F OtBu O 15 H 3 O+ CH3. Et 33 ...
elimination of methyl mercaptan to afford the guanidine ( 20 ). Reaction of 20 with the indole aldehyde ( 21 ) affords ( 22 ).^3 ...
NH CO 2 P NH 2 + 29 HO 2 C CO 2 P'' NHP' 30 NH CO 2 H HN CO 2 H O 31 The substrate arachidonic acid, which often leads to format ...
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