7 - Chlorotheophylline

Alkylation of chlorotheophylline with chloroacetonitrile gave 608 and cyclization with hydrazine gave [88CI(L)785] triazine derivative 609. Condensation of the latter with different aldehydes gave the corresponding hydrazones. 

Cafllon (Ravensberg)-corab. with phenmetrazine-8-chlorotheophyllinate wfm... 

Cafilon (Yamanouchi)-comb. with phenmetrazine-8-chlorotheophyllinate... 

Dimenhydrinate Dimenhydrinate (16.1.2) is a complex componnd of iV, iV-dimethyl (2-diphenyhnethoxy)ethylamine—diphenhydramine with 8-chlorotheophylline. While blocking the Hj receptor, dimenhydrinate simultaneonsly acts on the vomiting center [4,5]. 

Pharmacology Dimenhydrinate consists of equimolar proportions of diphenhydramine and chlorotheophylline. 

Chlorotheophylline reacted with the nitrilium imides generated in situ from amidrazones treated with triethylamine to give [l,2,4]triazolo[3,4 ]purines as single regioisomers in very high yield (Scheme 1) <2001JOC4055>. The... 

The reaction of 8-chlorotheophyllines with nitrilium imides to give [l,2,4]triazolo[3,4y]purines may be described as a [3+2] cycloaddition process <2001JOC4055> see Section 10.11.5.1. The purine bicycle has been prepared through the Diels-Alder-retro-Diels-Alder reaction of 2,4,6-tris(ethoxycarbonyl)-l,3,5-triazine with 5-amino-l-benzylimida-zole <1999JA5833> see Section 10.11.10.3. 

The unpleasant sedative CNS effect of most antihistamines, combined with their slight anticholinergic activity, is exploited for the prevention of motion sickness. Diphenhydramine (2.5), in the form of an 8-chlorotheophylline salt (dimenhydrinate, 4.148), is widely used for this purpose. The theophylline derivative was originally added to counteract the drowsiness produced by diphenhydramine, since it is a central excitant related to caffeine. 

IV-Chlorosuccinimide [128-09-6] M 133.5, m 149-150°. Rapidly crystd from benzene, or glacial acetic acid and washed well with water then dried in vacuo. [Phillips and Cohen JACS 108 2023 1986. 8-Chlorotheophylline [85-18-7] M 214.6, m 311°(dec). Crystd from water. 

Dim en hydrin a te. Dimenhydrinate [523-87-5] (Dram amine) (18) is a white crystalline, ododess powder that melts between 102 and 107°C. It is sparingly soluble in water, freely soluble in ethanol and chloroform, and sparingly soluble in diethyl ether. Dimenhydrinate is prepared by combining dimethylaminoethyl benzhydryl ester with 8-chlorotheophylline and refluxing in an isopropyl alcohol solution. The crystalline precipitate of dimenhydrinate that forms on cooling is collected by filtration, washed with cold ethyl acetate, and dried. 

Chemical Name 4-Diphenylmethoxy-l-methylpiperidine-, compd. with 8-chlorotheophylline (1 1)... 

In an attempt to compensate for the sedative side effect of this compound, a complex with 8-chlorotheophylline 40, dimen-hydrinate, was investigated. In addition to its antihistaminic quality it is also effective against travel sickness. 

Synonym. Phenmetrazine 8-Chlorotheophyllinate C,H,5N0,C7H7C1N402 = 391.9 CAS—13931-75-4 A white powder. 

Synonym. Promethazine Chlorotheophyllinate Proprietary Names. Avomine Meth-Zine. 

Phenmetrazine chlorotheophyllinate, 882 Phenmetrazine hydrochloride, 882 Phenmetrazine theoclate, 882 Phenobarbital, 883 Phenobarbital sodium, 883 Phenobm bitone, 25, 883 (metabolite), 771,923 therapeutic drug monitoring, 109 Phenobarbitone sodium, 883 Phenobarbitone, soluble, 883 Phenoctide, 830 Phenododecinium bromide, 570 Phenol, 884 (metabolite), 380 Phenolphthalein, 885 Phenomorphan, xvii Phenomycilline, 887 Phenoperidine, 885 Phenoperidine hydrochloride, 886 Phenopromini sulphas, 349 Phenopropazine, 599 Phenothiazine, 886... 

---