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The cyclic undecapeptide cyclosporin A (CsA) has a remarkable spectrum of diverse biological activities, including anti-inflammatory, antifungal, antiparasitic as well as immunosuppressive activities. However, the low water solubility of this drug is a ser ...
N-Substituted (3S,4S)- and (3R,4R)-pyrrolidine-3,4-diols 9 and 10, respectively, were derived from (+)-L- and (-)-D-tartaric acid, respectively. Compounds 9k, 91, and 9m with the N-substituents, BnNH(CH2)(2), 4-Phc(6)H(4)CH(2)NH(CH2)(2) and 4-ClC6H4CH2NH(C ...
Fully synthetic polymers were used for the prepn. of hydrogel beads and capsules, in a processing scheme that, originally designed for calcium alginate, was adapted to a "tandem" process, that is the combination a phys. gelation with a chem. crosslinking ...
The present invention relates to a process for preparing sulfonyl halides comprising the steps of a) reacting an enoxymetal, allylsilane or allylstannane compound, preferably in the presence of a diene, with sulphur dioxide and b) adding a suitable halogen ...
The reaction of the anilines RNH2 [R = C6H4(o-CN), C6H4(p-CN), C6H4(m-CN), C6H4(o-C6H5), C6F5 and C6H4(o-CF3)] with Ph2PCl and inorganic or organic bases in differing stoichiometry and in different solvents has been studied. The electronic properties and s ...
The conversion of 2,2-difluoro-1,3-benzodioxole, an exceptionally acidic arene, via a 4-lithiated intermediate into more than three dozen new derivs. was conceived as a case study. The lithiated species was trapped by C0-electrophiles (4-toluenesulfonyl az ...
This paper describes the synthesis of several novel water-soluble highly branched polypeptides. The synthesis starts with the ring-opening polymerization of ε-benzyloxycarbonyl-L-lysine N-carboxyanhydride (Z-Lys NCA) or ε-trifluoroacetyl-L-lysine N-carboxy ...
Trifluoromethoxy-substituted anilines undergo hydrogen/lithium permutation ("metalation") with optional site selectivity depending on the N-protective group employed. N-tert-Butoxycarbonyl-2- and -4-(trifluoromethoxy)aniline react with tert-BuLi at the n ...
The amino-amido-thiol AT (HS-(CH2)10-CO-NH-CH2-CH2-NH2)(HS-(CH2)10-CO-NH-CH2-CH2-NH2), adsorbed on Au(111), was studied by sum frequency generation (SFG) and IR reflection absorption spectroscopy in the CH2 stretching vibration region. The SFG and IR spect ...
