2-Hydroxy-1-propylamino

S)-A/-[2-[3-(2-cyano-phenoxy)-2-hydroxy-propylamino]-ethyl]-A/ -[4-(2-[ F]fluoroethoxy)-phenyl]-ur a 10... 

Recently, the 2-[ F]fluoroethylation of a phenolic desalkyl precursor based on the jSi-AR-selective antagonist ICI 89,406 was realized via a two-step synthesis starting with the [ F]fluorination of ethylene glycol di-p-tosylate. The radiosynthesis yielded (S)-A/-[2-[3-(2-cyano-phenoxy)-2-hydroxy-propylamino]-ethyl]-A/ -[4-(2-[ F]fluoroethoxy)-phenyl]-urea 10, representing a potent F-labeled high affinity / i-AR-selective radioligand with a / i-AR-selectivity of >40.000 (Fig. 15) [107],... 

Malonsaure [Azido-(3-hydroxy-propylamino)-methylen]- -methylester-nitril E15/1, 858 (N3 NH-R)... 

Ethoxycarbonyl-2-hydroxy-4-phenyl- 83 5-Ethoxycarbonyl-2-(3-hydroxy-propylamino)-4-phenyl- 65... 

The 1- and 3-(hydroxypropyl)-2-aminodihydroquinazolines are also cyclized to the angular and linear benzologue, respectively, by treatment with SOCI2. However, from 2-(3-hydroxypropyl-amino)quinazoline a mixture of (144) and (60) was formed in which (144) predominated (Equation (47)) <79CPB880>. Only the angular derivative was obtained from 6-chloro-2-(3-hydroxy-propylamino)-4-phenylquinazoline <73NKK1944>. 

The development of a NACE method, using 6-mono-deoxy-6-mono(3 -hydroxy)propylamino- p-CD (MMHP-... 

PYRROLEANDPYRROLEDERIVATIVES] (Vol20) (+)-N-(2-Hydroxy-3-[ql(4-hydroxyphenoxy)propylamino)ethyl morphine-4-caiboxamide... 

The use of selective P-antagonists for treatment of CHF has included the P -blocker metoprolol (Table 1) and results of clinical trials suggest long-term beneficial effects. Selective P -antagonists have also been tested, an example of which is xamoterol [81801 -12-9], C2 H25N20, which is (i)-A/-(2-hydroxy-3-(4-hydroxyphenoxy)propylamino)ethylmorphine-4-carboxamide. Xamoterol exhibits approximately 50% of the activity of isoproterenol, and serves to provide modest inotropic effects (128,129). 

CN l-[2-[2-hydroxy-3-(propylamino)propoxy]phenyl]-3-phenyl-l-propanone hydrochloride... 

Glennon RA et al. (1988) NAN-190 an cU ylpiperazine analog that antagonizes the stimulus effects of the 5-HTlA agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). Eur J Pharmacol 154(3) 339-341... 

Portas, C. M., Thakkar, M., Rainnie, D. McCarley, R. W. (1996). Microdialysis perfusion of 8-hydroxy-2-(di-n-propylamino)tetrahn (8-OH-DPAT) in the dorsal raphe nucleus decreases serotonin release and increases rapid eye movement sleep in the freely moving cat. J. Neurosci. 16, 2820-8. 

Bonaventure, P., Nepomuceno, D., Kwok, A. et al. Reconsideration of 5-hydroxytryptamine (5-HT)7 receptor distribution using [3H]5-carboxamidotryptamine and [3H]8-hydroxy-2-(di-n-propylamino)tatraline Analysis in brain of 5-HT 1A knock-out and 5-HT1A,1B double knock-out mice. /. Pharmacol. Exp. Ther. 302 240-248, 2002. 

Acebutol Acebntol is 3 -acetyl-4 -[2-hydroxy-3-(Ao-propylamino)propoxy] butyranilide (12.1.6) [9,10]. 

Atenolol Atenolol is 2-[4 [2-hydroxy-3-(tT<9-propylamino)propoxy]phenyl]acetamide (12.1.7). The synthesis of this drug is described in Chapter 12. 

Carli M, Tranchina S, Samanin R 8-Hydroxy-2-[di-n-propylamino)tetralin, a 5-HTj, receptor agonist, impairs performance in a passive avoidance task. Eur J Pharmacol 211 227-234, 1992... 

Tricklebank M, Forler C, Fozard J The involvement of subtypes of the 5-HTl receptor and of catecholaminergic systems in the behavioural response to 8-hydroxy-2-(di-n-propylamino) tetralin in the rat. Eur J Pharmacol 106 271-282, 1984... 

Applications. Various N-derivatives of amino acids (qv) are resolvable on BSA columns. These A/-amino acid derivatives include benzenesulfonyl-, phthalimido-, 5-dimethylamino-l-naphthalenesulfonyl- (DANSYL-), 2,4-dinitrophenyl- (DNP-), and 2,3,6-trinitrophenyl- (TNP-) derivatives (30). Amines such as Prilocain, (+)-2-(propylamino)-0-propiono-toluidide, a local anesthetic (Astra Pharm. Co.), are also resolved on BSA. The aromatic amino acids DL-tryptophan, 5-hydroxy-DL-tryptophan, DL-kynurenine [343-65-7], C10H12N2O3, and 3-hydroxy-m.-kynurenine [484-78-6], and dmgs such as warfarin, phenprocoumon, and benzodiazepine derivatives can be separated on BSA as well. 

OHDPAT, 8-hydroxy-2(di- -propylamino)tetralin ACPD, trans-1 -amino-cyclopenty 1 -1,3 -dicarboxylate AMP A, DL-cr-amino-3-hydroxy-5-methylisoxazole-4-propionate BIMU8, [endo-A-8-methyl-8-azabicyclo(3.2.1)oct-3-yl]-2,3-dihydro-3-isopropyl-2-oxo-177-benzimidazol-l-carboxamide hydrochloride CGP 35348, 3-aminopropyl(diethoxymethyl)phosphinic acid CNQX, 6-cyano-7-nitroquinoxaline-2,3-dione CP 99994, (+)-(2 , 3A)-3-(2-methoxybenzylamino)-2- ... 

Atenolol is 4-/2-hydroxy-3-/(l-methylethyl)-amino/-propoxy/-benzenacetamide and is also known as 2-/p-/2-hydroxy-3-(isopropylamino)propoxy/phe-nyl/acetamide or l-p-carbamoylmethylphenoxy-3-iso-propylamino-2-propanol. 

Dihydro-2-(2-methoxy)ethyl-4-propylamino-2H-thieno[3,2-e]-l,2-thiazine-6-sulfonamide-l,1-dioxide hydrochloride was obtained by the reaction of 3,4-dihydro-4-hydroxy-2-(2-methoxy)ethyl-2H-thieno[3,2-e]-l,2-thiazine-6-sulfonamide-1,1-dioxide in THF containing triethylamine with tosyl chloride at -16°C and the next stirring for 18 hrs at room temperature. After which time the mixture was cooled to 0°C and propylamine was added, the desired product (0.57 g, 46%) was obtained m.p. 178°-181°C. 

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