公开(公告)号：BG107390A

公开(公告)日：2004-06-30

申请号：BG10739002

申请日：2002-12-16

Applicant: BALKANFARMA DUPNITSA AD

Inventor： STANEVA TINKA D ,  NACHEVA ELIZABET B ,  LAZAROV VLADIMIR K ,  BACHEVA BOJKA L ,  KATSARSKI DIMITAR E

IPC: A61K31/445 ,  C07D211/14

Abstract: The invention relates to a method for the preparation of 2-[4-[2-(1-piperidinyl)ethoxy] benzoyl] benzoic acid methyl ester hydrochloride having antispasmolytic activity and strong local anaesthetic effect and is used as antispasmolytic component in medicamentous compositions in combination with analgetics. By the method, a high purity and high yield product is turned out in reaction between phenol and dichlorethane, acylation of the phenyloxyethylchloride produced and subsequent amination with piperidine in aqueous-alkaline medium at 100 degrees C of an influx. After the water distillation the remainder is cooled to room temperature and is esterified with methanol and sulphuric acid at 65 to 75 degrees C. After the elimination of the methanol excess, the remainder of the reaction mixture is diluted in water and is neutralized to pH 7-8 at continuous cooling. The ester produced is extracted by dichlorethane, the extract is evaporated, and the residue is dissolved in acetone, hydrochloric acid is added, and the reaction mixture is cooled to 0-5 degrees C. The sediment produced is filtered, washed in acetone, is dried and purified in ethanol. The purified product crystallizes by the addition of acetone and cooling to 0-5 degrees C and is then dried. 2 claims

公开(公告)号：BG63360B1

公开(公告)日：2001-11-30

申请号：BG10361199

申请日：1999-07-28

Applicant: BALKANFARMA DUPNITSA AD

Inventor： PARALANOVA DANIELA I ,  STANEVA TINKA D ,  KAFEDZHIJSKI STEFAN K

IPC: A61K31/00 ,  A61K31/14 ,  C07C209/12 ,  C07C211/63

Abstract: The method finds application in the chemical industry. The cetyl-trimethyl ammonium bromide is used as a disinfectant in the human and veterinary medicine, as birth control means, as well as in testing of foods in the food industry, By the method the cetyl-trimethyl ammonium bromide is produced with high yield and purity in reaction with cetyl bromide, produced in the bromation of cetyl alcohol with dual residue of hydrogen bromide in sulphur-acid medium with alcohol solution of trimethylamine. After the end of the process the alcohol is distilled under vacuum, the residue is cooled and mixed with acetone with intensive agitation. The mixture produced is filtered, and the separated sediment of the cetyl-trimethyl ammonium bromide is dried. 1 claim

公开(公告)号：BG63941B1

公开(公告)日：2003-07-31

申请号：BG10254798

申请日：1998-06-17

Applicant: BALKANFARMA DUPNITSA AD

Inventor： STANEVA TINKA D ,  LAZOV VLADIMIR K ,  STANEV STANCHO R ,  DIMITROVA-BACHEVA BOJKA L ,  BOTSEVA ADELINA V ,  KAFEDZHIJSKI STEFAN K

IPC: C07D211/10 ,  C07D211/30 ,  C07D211/74

Abstract: The 2,2,6,6-tetramethyl-4-oxopiperidine p-toluenesulphonate is used in medicine as antidepressive and antineurotic means. By the method p-toluenesulphonic salts of 2,2,6,6-tetramethyl-4-oxopiperidine, also known as triacetonamine is produced at high yields and purity in a reduced and simplified process in catalytic condensation of acetone with ammonia. The reaction occurs at temperature range from -15 to +15 degrees C at continuous agitation and slow acetone saturation with gaseous ammonia, until a ratio between them of 1.5:1 to 1:1.5 is achieved. In the addition to the acetonine-containing reaction medium of additional catalyst quantities and 0.1-1 ml siccative, the acetonine is converted into triacetonamine. The triacetonamine produced, without being isolated from the reaction mixture, is settled as a salt at the addition of p-toluenesulphonic acid. 5 claims

公开(公告)号：BG103611A

公开(公告)日：2001-02-28

申请号：BG10361199

申请日：1999-07-28

Applicant: BALKANFARMA DUPNITSA AD

Inventor： PARALANOVA DANIELA I ,  STANEVA TINKA D ,  KAFEDZHIJSKI STEFAN K

IPC: A61K31/00 ,  A61K31/14 ,  C07C209/12 ,  C07C211/63

Abstract: The invention relates to a method for the synthesis of cetyl-trimethyl ammonium bromide with the formula The compound has strong bacterial effect and finds wide application in hygiene, birth control and foodstuffs testing for the content of dyestuffs. The cetyl-trimethyl ammonium bromide is produced by the reaction between cetylbromide and trimethylamine in alcohol medium with an yield of about 90 %. Each of the initial reagents is being produced at a high yield (85 %) and purity (98 %) and is being used for the synthesis of the end compound. The cetylbromide is produced from cetyl alcohol and hydrogen bromide, and the trimethylamine from paraformaldehyde and ammonium bromide. The methods for the synthesis of the intermediate products and the end compound are industrially applicable. 3 claims

公开(公告)号：BG105640A

公开(公告)日：2003-01-31

申请号：BG10564001

申请日：2001-06-22

Applicant: BALKANFARMA DUPNITSA AD

Inventor： STANEVA TINKA D ,  KAFEDZHIJSKI STEFAN K ,  NACHEVA ELIZABETA B ,  PARALANOVA DANIELA I ,  STANEV STANCHO R ,  KATSARSKI DIMITAR E

IPC: C07C255/49

Abstract: The method is used in the pharmaceutical industry for the production of 4-hydroxy-3-iodo-5-nitrobenzonitrile, known by its generic name of Nitroxynil, which is used in the veterinary pharmaceutical practice for the treatment of helminthic infections. The compound has high yield and purity and is produced by the method of nitration of 4-hydroxybenzonitrile with water solution of sodium or ammonium nitrate, in saline-acidic medium at 80 degrees C and continuous agitation. The 4-hydroxy-5-netrobenzonitrile produced is iodized at 80 to 110 degrees C, after which the reaction mixture is cooled to 10-15 degrees C. The precipitation of 4-hydroxy-3-iodo-5-benzonitrile is filtered, rinsed in water, re-crystallized in ethanol and is dried. 3 claims

公开(公告)号：BG102547A

公开(公告)日：2000-04-28

申请号：BG10254798

申请日：1998-06-17

Applicant: BALKANFARMA DUPNITSA AD

Inventor： STANEVA TINKA D ,  LAZOV VLADIMIR K ,  STANEV STANCHO R ,  DIMITROVA-BACHEVA BOJKA L ,  BOTSEVA ADELINA V ,  KAFEDZHIJSKI STEFAN K

IPC: C07D211/10 ,  C07D211/30 ,  C07D211/74 ,  A61K31/445

Abstract: The invention relates to a method for the preparation of 2,2,6,6-tetramethyl-4-oxopiperidine p-toluenesulphonate showing antidepression and antineurotic effect. The compound has the general formula The method consists of consecutive production of triacetonamine from acetone and gaseous ammonia. Additional quantity of acetone and a catalyst is added and the compound becomes 2,2,6,6-tetramethyl-4-oxopiperidine which, without being isolated, settles as a salt of the p-toluenesulphonic acid. 4 claims