专利号:US-3948883-A 优先权日:1974-11-11 标题:Synthesis of purine nucleosides 发明人:RANGANATHAN RAMACHANDRAN S 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:A desired purine-containing nucleoside is synthesized by condensing a nitropyrimidine with a thionoxazolidine that is an adduct of a sugar unit and an oxazolidine ring unit having two adjacent carbon atoms in common. Prior to condensing the thionoxazolidine is converted to the bromo-mercuric derivative to promote the reaction at the nitrogen site. The N-alkylated condensation product is reduced to produce an amino-pyrimidine nucleoside which is then heated under conditions to cyclize it to a mercapto-purine nucleoside. The cyclized product is finally desulfurized to produce the desired purine-containing nucleoside. The compounds are useful as anti-viral agents.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
专利号:CN-86102542-A 优先权日:1986-10-20 标题 :Synthesis of Sugar-N-(aminopyrimidinyl)-oxazolidine-2-thione
专利号:CN-1021736-C 优先权日:1986-10-20 标题 :Synthesis method of glucoiso-N-(aminopyrimidinyl)-oxazolidine-2-thione