The preparation of three series of esters and phenylurethanes of pyr-Their configurations are rolidine alcohols as local anathetics is described. discussed on the basis of their pK, values.
The shape of a titration curve contains useful information, which may be extracted in terms of orthogonal polynomial coefficients. In this way, it is possible to (i) distinguish a monobasic acid from a polybasic acid, having groups of closely similar strength; (ii) detect acid‐base impurities in acids and bases, and (iii) study medium effects. The choice of polynomial, range, number of points and experimental conditions are discussed. Using twelve point polynomials and equipment of modest performance, the Pi coefficient (for the central half of a monobasic acid titration curve) can be measured with a relative standard deviation of 0·58.
The configurations of the two isomers, β‐eucaine (benzamine hydrochloride B.P.C. 1954) and β‐isoeucaine have been deduced. As a result of a study of the nuclear magnetic resonance spectra and of catalytic hydrogenation and oxidation, the α‐form has been assigned an equatorial hydroxyl group on C‐4 and the β‐form an axial hydroxyl group in this position.
Three new pyrrolidylalkanol esters, 2‐p‐methoxybenzoyloxymethyl‐1‐methyl‐, 2,5‐di(p‐methoxybenzoyloxymethyl)‐1‐methyl‐ and 2,5‐di(2‐ p‐methoxybenzoyloxypropyl)‐1‐methyl‐pyrrolidine have been prepared and tested as local anaesthetics. The activity of the last compound has been shown to be almost identical with that of cocaine by the intracutaneous route, though it is without action on the cornea.
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