Solid-Phase Synthesis of Piperidines by N-Acyliminium Ion Chemistry
摘要:
An efficient solid-phase procedure for the synthesis of a number of 2-substituted piperidines is reported. Starting from solid-supported carbamate-tethered delta-amino acetals, 2-benzotriazolyl-substituted (Bt-substituted) piperidines were obtained by acid-induced ring-closure followed by trapping of the transient N-acyliminium ions with benzotriazole. These 2-Bt-substituted piperidines were then used as precursors for the successful introduction of several C-nucleophiles by N-acyliminium. ion chemistry. (C) Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002.
Triflic acid-mediated phenylation of N-acylaminoalkyl diethylacetals and N-acyl-2-phenyl cyclic amides
作者:Frank D. King、Stephen Caddick
DOI:10.1039/c0ob01149e
日期:——
The reaction of N-acylaminoalkyl diethylacetals with triflic acid in benzene gave N-acylamino-diphenylalkyls. The proposed intermediates are the N-acyl-2-phenyl cyclic amides, which themselves are similarly converted to N-acylamino-diphenylalkyls.
MENTHYL CARBAMATE COMPOUNDS AS SKIN AND/OR HAIR LIGHTENING ACTIVES
申请人:Vielhaber Gabriele
公开号:US20130129646A1
公开(公告)日:2013-05-23
The present invention relates to the cosmetic, dermatological or pharmaceutical (therapeutic) use of compounds of formula (I) or a cosmetically acceptable salt of a compound of formula (I) or a mixture containing two or more of these compounds or the salts thereof
wherein
R
1
denotes hydrogen or an organic radical having 1 to 14 carbon atoms,
R
2
denotes an organic radical having 1 to 14 carbon atoms,
and
wherein optionally R
1
and R
2
are covalently bonded to one another, preferably so that a 3 to 8 membered ring is formed,
for the lightening of skin and/or hair.
The invention further relates to compositions and cosmetic, dermatological or pharmaceutical preparations (compositions) comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods. The invention further relates to compounds of formula (I) as a drug, their use for the preparation of a pharmaceutical composition for lightening human skin and/or hair and to certain novel compounds of formula (I).
A simple one pot procedure for the generation of homoallylic alcohols from acetals and amino acetals
作者:Adam McCluskey、Debra M Mayer、David J Young
DOI:10.1016/s0040-4039(97)01106-4
日期:1997.7
Treatment of acetals (1 and 2) and amino acetals (3–5) with either trifluoroacetic acid (TFA) or silica gel followed by tetraallyltin gave excellent yields of the corresponding homoallylic alcohols (68 – 100%).
A novel synthesis of (±)-harmacine and (±)1,2,3,4,6,7,12,12b-octahydroindole[2,3-a]quinolizine
作者:Frank D. King
DOI:10.1002/jhet.5570440634
日期:2007.11
A three-step synthesis of (±)-harmacine is described from the readily available 4,4-diethoxybutan-1-amine via an acid-mediated acyl iminium ion cyclisation. The synthesis of the homologous (±)1,2,3,4,6,7,12,12b-octahydroindole[2,3-a]quinolizine from 5,5-diethoxypentan-1-amine is also described. Although similar, the two systems required very different cyclisation conditions.
从容易获得的4,4-二乙氧基丁烷-1-胺经酸介导的酰基亚胺离子环化反应,描述了(±)-甜菜碱的三步合成法。还描述了由5,5-二乙氧基戊丹-1-胺合成同源的(±)1,2,3,4,6,7,12,12b-八氢吲哚[2,3- a ]喹诺嗪。尽管相似,但这两个系统需要非常不同的环化条件。