Über Alkylenimin‐Derivate. 12. Mitteilung. Piperidin‐Derivate mit zentralerregender Wirkung II

Abstract

The study of the time dependance of this thermal effect (Gough-Joule effect) shows that the crystallization of rubber after extension is slow and may be studied during several hours, the final stage of crystallization being probably a first order reaction whose velocity constant is nearly independant of strain and has a low temperature coefficient. On the other hand, the fusion following the release of the applied tension is rapid.

Biological Activity in Compounds Possessing Thiophen Rings

“…The hydrochloride salt of 2-thienylmethyl-isothiourea was found to produce a fall in blood pressure and heart rate and to depress respiratory movements in chloralosed cats,350 and several substituted 2-methylpiperidines including two thienyl derivatives were found to possess a stimulating effect on the CNS. 351 Some thiophen compounds related to 1-phenylindan proved to be without significant analgesic activity.352 Herz's group has been actively engaged in the preparation of thiophen analogues of various isoquinolines,353 and some of the compounds of this series may well have interesting biological properties.…”

Alkylation of α-tert-butoxycarbonylamino ketone enolate anions. A useful synthesis of α-alkyl-α-amino ketones, 2-acylpyrrolidines, and 2-acylpiperidines

“…gave the cyclic a-amino ketones 7 (Table 2). Given the ready availability of 2, this process constitutes a very useful route to such compounds for which few syntheses have been reported (21)(22)(23).…”

Central Stimulants. α,α-Disubstituted 2-Piperidinemethanols and 1,1-Disubstituted Heptahydroöxazolo [3,4-a]pyridines

“…The desired product (Table I, 30A) from the reaction involving p,p'- (T able I, 36C) was prepared by method H. After this work had been completed, a similar preparation of this compound was reported. 8 The synthesis of the N-methyl derivative of 36C has also been described.16 These papers also reported the reaction of 2-benzoylpiperidine8 and its N-methyl deriva-tive16 with 2-thienylmagnesium bromide to produce the corresponding piperidinemethanols.…”

“…The reported melting point is 123-125°. 8 Hydrogenation of 2-Pyridinemethanols (Method I), (a) General Procedure.-A mixture of 0.2 mole of the substituted pyridinemethanol hydrochloride, 200 ml. of methanol and 0.6-0.8 g. of platinum oxide catalyst was shaken with hydrogen at 3 to 4 atmospheres pressure in a Parr hydrogenation apparatus until the theoretical amount (0.6 mole) of hydrogen had been absorbed.…”