Organic Chemistry of Drug Synthesis. Volume 7
the carbonyl group in 2 with hypochlorite followed by reaction with thionyl chloride leads to the acid chloride ( 3 ). Condensat ...
Red blood cells in patients afflicted with sickle-cell anemia show a reduced capacity for holding oxygen. The adventitious disco ...
The synthesis of the first of these starts with the formation of the enamide ( 18 ) from tyrosine ( 16 ) and 2-benzoylcyclohexan ...
is used to alkylate the phenol group onp-hydroxybenzaldehyde ( 23 ). Condensation of the aldehyde group in 24 with glycine methy ...
Cl + O O O AlCl 3 Cl CO 2 H O 31 32 33 Cl^34 CO 2 H O S C 6 H 5 SH Research on the prostaglandins several decades ago revealed a ...
Saponification of the methyl ester followed by hydrogenolysis of the benzyl ether completes the synthesis of the leukotriene B 4 ...
ethanolamine moiety present in the great majority of compounds that act on adrenergic receptors. Thus,solabegron( 56 ) is obtain ...
then treated with ethyl oxalate ( 64 ) to afford the oxamic ester 65. The carbonyl group is then reduced to the corresponding al ...
chromatography. Catalytic hydrogenation of the appropriate diastereomers leads to scission of the benzylic carbon-to-nitrogen bo ...
4. COMPOUNDS RELATED TO ARYLSULFONIC ACIDS The title for this section aptly illustrates the almost arbitrary criteria used to gr ...
Elastase is an inflammatory protease associated with lung injury caused by infection or any of a number of other tissue insults. ...
Construction of the thiomorpholine moiety starts by protection of the car- boxylic acid in penicillamine ( 102 ) by reaction wit ...
115 with methylamine gives intermediate 116. Acylation of the secondary amine with pivaloyl chloride affords the corresponding a ...
HO OCNSO 2 Cl SO O 2 H 2 O HCl CH 2 Cl KCN CN OH– CO 2 H OCN SO O 2 H 2 N SO O 2 HN 118 119 120 121 122 123 124 125 O CH 2 =O Th ...
sulfenic acid ( 128 ). Alkylation by means of base and methyl bromide gives the corresponding aryl methyl sulfone ( 129 ). The c ...
from 2-chloroethyl diidopropyl amine ( 136 ) to afford the benzhydrol ( 137 ). Hydrogenolysis over palladium would then afford t ...
proceeds to give exclusively to the (E) olefin isomer. Acid hydrolysis removes the acetyl protection. Reaction of that intermedi ...
HO 2 C CO 2 H O 151 + N CH=O 152 HO 2 C CO 2 H O O N N 153 154 O N N 155 H 2 C 6 H 5 CH 2 NH 2 NaBH 3 CN HN N N 156 N N N O 157 ...
removal of chromium by iodine gave the product in high yield. Removal of thet-BOC protecting group with trifluoroacetic acid (TF ...
N CO 2 C 2 H 5 167 NC N + Base O NC H+ N O N O Br 2 Br N+ O N H 2 O 168 169 170 173 172 171 N NH 175 OCH 3 H3C CH 3 H 2 N OCH 3 ...
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