63608-15-1Relevant articles and documents
Remote C(sp3)-H Oxygenation of Protonated Aliphatic Amines with Potassium Persulfate
Lee, Melissa,Sanford, Melanie S.
, p. 572 - 575 (2017/02/10)
This letter describes the development of a method for selective remote C(sp3)-H oxygenation of protonated aliphatic amines using aqueous potassium persulfate. Protonation serves to deactivate the proximal C(sp3)-H bonds of the amine substrates and also renders the amines soluble in the aqueous medium. These reactions proceed under relatively mild conditions (within 2 h at 80 °C with amine as limiting reagent) and do not require a transition metal catalyst. This method is applicable to a variety of types of C(sp3)-H bonds, including 3°, 2°, and benzylic C-H sites in primary, secondary, and tertiary amine substrates.
Process for the preparation of 4-methylenepiperidine
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, (2008/06/13)
PCT No. PCT/JP96/02810 Sec. 371 Date Mar. 26, 1998 Sec. 102(e) Date Mar. 26, 1998 PCT Filed Sep. 26, 1996 PCT Pub. No. WO97/11939 PCT Pub. Date Apr. 3, 1997A process for preparing 4-methylenepiperidine having a formula (VII): which comprises reacting an isonipecotate having a formula (I): wherein R1 is methyl group or ethyl group, with an acylating agent having a formula (II): R2X or a formula (II'): (R2)2O wherein R2 is benzoyl group or acetyl group and X is chlorine atom or bromine atom, in the presence or the absence of a base, reducing the resulting ester having a formula (III): wherein R1 and R2 are the same as defined above, with sodium borohydride or lithium borohydride in an organic solvent containing methanol, reacting the resulting alcohol with a halogenating agent without any solvent or in an organic solvent in the presence or the absence of a base, reacting the resulting halide with a dehydrohalogenating agent in an organic solvent and hydrolyzing the resulting methylene compound having a formula (VI): wherein R2 is the same as defined above, with a strong alkaline in water or an organic solvent containing water.
4-Phenoxymethyl-piperidines
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, (2008/06/13)
4-Phenoxymethyl-piperidines of the formula STR1 wherein R is hydrogen, halogen, nitro, lower alkyl or lower alkoxy, in the form of the free base or an acid addition salt, are provided and they are useful as intermediates in the production of anti-hypertensive agents through condensation with (a) propyl chloride and then with an adenine, or (b) a propyl indole.