2- Hydroxy-1-piperidino

Janssen, P. (Janssen) 2,2-Diaryl-4-(4 -aryl-4 -hydroxy-piperidino)-butyramides, US 3 714 159,1973. 

Hydroxy-piperidino-phosphoryl)- XII/2, 402 O-(Hydroxy-propytoxy-phosphoryl)- XII/2, 272 5 -0-(Hydroxy-valyl-phosphoryl)- XII/2, 559 2, 3 -0-Isopropyliden-5 -0-phospho- XII/2, 179 2 -0-Phospho- XII/2, 201... 

Hashimoto K, Fujita N, Tanaka T, Kido M (1995) 6-ethyl-9-fluoro-6,7-dihydro-8-(4-hydroxy-piperidino)-5-methyl-1-0X0-l/f,5/f-benzo[i/ qumoh-zme-2-caiboxyUc add. Acta Crysbillogr Sect C 51 519-521... 

The initial steps involve reacting benzyl chloride with 4-hydroxy propiophenone. The benzyl-oxypropiophene thus obtained is first brominated and then reacted with 4-benzylpiperidine to give 1-(p-benzyloxyphenyl)-2-(4-benzyl-piperidino)propan-1-one. 

Likewise, amine functions on the azepine ring at an unsaturated carbon center behave as enamines and undergo hydrolysis under both acid and alkaline conditions to the benzazepinones.15,64 8084 However, hydrolysis of dimethyl l-acetyl-5-piperidino-l//-l-benz-azepine-3,4-dicarboxylate(18) yields not the benzazepinone but the tautomeric 5-hydroxy derivative 19.13 Presumably, the enol form is stabilized by intramolecular hydrogen bonding. 

Das ziemlich einfach herstellbare 1 -Hydroxy- 1-piperidino-cyclopropan kann in Gegen-wart von Titan(IV)-chlorid in einer Variante der Mannich-Reaktion als Aquivalent von Cyclopropanon/Piperidin dienen nach der anzunehmenden in-situ-Umwandlung in 1-Cyclopropyliden-piperidinium-chlorid erfolgen Reaktionen z.B. mit 1-Trimethylsiloxy-cyclohexen zu 2-Oxo-l-(l-piperidino-cyclopropyl)-cyclohexan (63%) und mit 1-Methyl-pyrrol bzw. Indol zu l-Methyl-2-( 1-piperidino-cyclopropyl)-pyrrol (65%) bzw. 3-(l-Pipe-ridino-cyclopropyl)-indol (84%)2 ... 

Ethyl l-oxo-6-piperidino-l//-pyrimido[l,2-a]quinoline-2-carboxylate showed potent in vitro anticoccidial activity (92AAC2338). anhydro-1,3-Diethyl-2-hydroxy-4-oxo-4//-pyrimido[2,l-a]isoquinolinium hydroxyde (318) exhibits nonselective Ar and A2-adenosine receptor activities (84JMC1364) and proved to be an inhibitor of cyclic-AMP phosphodiesterase (81JMC1284). 8,9,10,ll-Tetrahydro-3-(l//-5-tetrazolyl)-4//-pyrimido[2,l-a]iso-quinolin-4-one exhibits antiulcer activity (84USP4457932). 

BUTYROPHENONE, 4 -FLUORO-4-(4-HYDROXY-4-(alpha,alpha,alpha-TRIFLUORO-m-TOLYL)PIPERIDINO)-... 

To a mixture of 4.2 g (0.0083 mole) of 4 -tert-butyl-4-[4-(a-hydroxy-a-phenylbenzyl)piperidino]-butyrophenone hydrochloride and 0.54 g (0.01 mole) of sodium methoxide in 25 ml of methanol is added 2.16 g (0.04 mole) of potassium borohydride. The reaction mixture is stirred overnight, diluted with water and the methanol removed under reduced pressure. The remaining material is extracted with chloroform, washed with water, dried over magnesium sulfate and filtered. The filtrate is concentrated, and the residue is recrystallized from acetone-water to give 4-[a-(p-tert-butylphenyl)-a-hydroxybenzyl]-a-phenyl-l-piperidinebutanol, melting point 161°-163°C. 

One of the first reports concerning the oxidative amination in quinazolines is the Cun-catalyzed amination of 6-hydroxy-2-phenylquinazo-line with piperidine and air. It provides 8-piperidino-2-phenylquinazoline 5,6-quinone (Scheme 19) (71KGS283, 71 KGS 1698). 

Hydroxy-pentamethoxy- E2, 831 Hydroxy-pentaphenoxy- E2, 831 Morpholino-pentachlor- XII/2, 989 Pentachlor-phenoxy- XII/2, 983 Pentachlor-piperidino- XII/2, 989... 

A number of quaternary 3-hydroxypyridinium chlorides (11) and a,co-bis(3-hy-droxypyridiniumo)alkane dichlorides (12) (as their betaines) have been hydrogenated to the corresponding piperidine derivatives over Rh-C as the catalyst.47 A typical run with the compound 11, R = / -chlorobenzyl, is shown in eq. 12.32. When platinum oxide was employed as the catalyst with the compound 12, n = 4, hydrogenolysis to yield l,4-bis(l-piperidino)butane took place. 3-Hydroxy-6-propylpyridine, however, was hydrogenated to 3-hydroxy-6-propylpiperidine in a 96% yield over platinum oxide in acetic acid at 20°C and 0.3 MPa H2.48... 

E21d, 4070 (Oxo - H/OH) Peroxid tert.-Butyl-(piperidino-methyl)- E13/1, 615 (NH + CH20 + R-O-OH) Propansaure 2-Hydroxy-2-methyl- -diisopropylamid E19d, 661 (H - Li/+ Keton)... 

Bicy clo 4.1. OJheptan 7-Hydroxy-7-piperidino- E17b, 1594/1596 (NR2 - OH) 7-Methyl-7-morpholino- E17b, 1586 (OR - CHj)... 

Hydrazin 2-(3,5-Dibrom-2-hydroxy-benzyliden)-l-(piperidino-methylen)- E14b, 671 (Hydraz-onid-Bildung)... 

Phthalazin 4-Hydroxy-1 -(piperidino-amino)- E16a, 791 (aus Phthal-imid-hydrazonid)... 

SYNS 4 -FXUORO-4-(4-HYDROXY-4-(a,a,a-TRIFLU-ORO-m-TOLYL)PIPERIDINO)BUTYROPHENONE 4-FLUORO-4,4-IDROSSI-4-(m-TRIFLUOROMETIL-FENTL)-PIPERIDINO-BL TIRROFENOKE (ITALIAN) l-(4-... 

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