Patent
Process for the preparation of condensed as-triazine derivatives
| العنوان: | Process for the preparation of condensed as-triazine derivatives |
|---|---|
| Patent Number: | 4,871,846 |
| تاريخ النشر: | October 03, 1989 |
| Appl. No: | 07/043,600 |
| Application Filed: | April 28, 1987 |
| مستخلص: | A process for the preparation of condensed as-triazinium derivatives of the formula I ##STR1## and isomers thereof, wherein R.sub.1 inter alia is an alkyl group, R.sub.2 inter alia is hydrogen or an alkyl group and R.sub.3 is hydrogen and where Z is a group of the formula a or b ##STR2## which comprises reacting a compound of the formula II ##STR3## where Y is a group of the formula c or d ##STR4## with a compound of the formula IIa [equation included] in the presence of a dehydrating agent. The advantage of the process is that it consists of fewer reaction steps and provides higher yields than the known methods. The compounds of formula I are pharmaceutically active known derivatives. |
| Inventors: | Batori, Sandor (Budapest, HUX); Hajos, Gyorgy (Budapest, HUX); Messmer, Andras (Budapest, HUX); Benko, Pal (Budapest, HUX); Pallos, Laszlo (Budapest, HUX); Petocz, Lujza (Budapest, HUX); Grasser, Katalin (Budapest, HUX); Kosoczky, Ibolya (Budapest, HUX); Szirt nee Kiszelly, Eniko (Budapest, HUX) |
| Assignees: | EGIS Gyogyszergyar (Budapest, HUX) |
| Claim: | What we claim is |
| Claim: | 1. The process for the preparation of a condensed as-triazine derivative of the formula I ##STR15## and isomers thereof where |
| Claim: | R.sub.1 is C.sub.1-10 alkyl, phenyl or naphthyl, wherein the two latter groups may optionally bear one or more identical or different halo, nitro, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s); |
| Claim: | R.sub.2 is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, phenyl or naphthyl, wherein the two latter groups may optionally bear one or more identical or different halo, nitro, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s); |
| Claim: | R.sub.3 is hydrogen; |
| Claim: | Z is a group of the formula (a) ##STR16## and |
| Claim: | A.sup.- is an anion |
| Claim: | which comprises: reacting a compound of the formula II ##STR17## where Y is a group of the formula c or d ##STR18## with the compound of the formula IIa [equation included] |
| Claim: | in the presence of a dehydrating agent. |
| Claim: | 2. The process of claim 1, wherein the reaction is carried out in an inert organic solvent. |
| Claim: | 3. The process of claim 1, wherein the dehydrating agent is a Lewis acid or a phosphorous oxyhalide. |
| Claim: | 4. The process of claim 1, wherein the dehydrating agent is titanium tetrachloride, aluminum chloride, boron trifluoride or phosphorous oxychloride. |
| Claim: | 5. The process of claim 1, wherein R.sub.1 is 4-chloro-phenyl, R.sub.2 and R.sub.3 are hydrogen and Z is a group of the formula (a). |
| Claim: | 6. The process of claim 1, wherein 1-hydroxy-1-(4-chlorophenyl)-1,2-dihydro-as-triazino[6,1-a]isoquinolinium salts are prepared. |
| Current U.S. Class: | 544/183 |
| Current International Class: | C07D25308 |
| Patent References Cited: | 4419355 December 1983 Kosoczky et al. 4602018 July 1986 Messmer et al. 4697013 September 1987 Messmer et al. |
| Primary Examiner: | Ford, John M. |
| Attorney, Agent or Firm: | Keil & Weinkauf |
| رقم الانضمام: | edspgr.04871846 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |