摘要:
Fungicidal compounds useful for the control of plant mildews are 4-alkyl-2,6-dinitrophenyl esters wherein the 4-alkyl group is selected from 1-ethyl-n-hexyl, 1-n-propyl-n-hexyl, 1-n-butyl-nhexyl, 1-n-pentyl-n-hexyl, 1-ethyl-n-pentyl, 1-n-propyl-n-pentyl, 1-n-butyl-n-pentyl and 1-n-propyl-n-butyl.
摘要:
An osmotic device that, following the imbibement of water vapor, provides for the controlled release of a beneficial agent to an aqueous environment. The device comprises a hydrophilic formulation including a beneficial agent, and if needed, an osmagent, surrounded by a wall. The wall is formed at least in part of a semipermeable hydrophobic membrane having an average pore size between about 0.1 .mu.m and 30 .mu.m. The pores are substantially filled with a gas phase. The hydrophobic membrane is permeable to water in the vapor phase and the hydrophobic membrane is impermeable to an aqueous medium at a pressure less than about 100 Pa. The beneficial agent is released, for example, by osmotic pumping or osmotic bursting upon imbibement of sufficient water vapor into the device core. These devices minimize incompatibilities between the beneficial agent and ions (such as hydrogen or hydroxyl) or other dissolved or suspended materials in the aqueous medium, since contact between the beneficial agent and the aqueous medium does not occur until after the beneficial agent is released. This results from the semipermeable membrane's selective permeability for water vapor. In addition, the high water fluxes attendant with these vapor-permeable membranes facilitate the delivery of beneficial agents having low solubilities, and the delivery of high dosages of beneficial agents.
摘要:
The intermediate ##STR1## wherein R is a lower alkyl group, is used to prepare a N-alkyl-3,4-dialkyl-2,6,-dinitro-aniline in a relatively simple, inexpensive and safe fashion, and with a high yield.
摘要:
A compound according to formula 1 ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, carbamoyl which is substituted by an alkyl of 1 to 4 carbon atoms, alkylcarbonyl of 2 to 5 carbon atoms or phenyl carbonyl, X represents halogen nitro or cyano and R.sub.3 represents ##STR2## wherein R.sub.4 represents cyano or alkylcarbonyl of 2 to 5 carbon atoms and R.sub.5 represents carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms or which is substituted with hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable esters and salts thereof, and a pharmaceutically acceptable carrier therefor, as well as pharmaceutical compositions containing said compounds as COMT inhibitors.
摘要翻译:根据式1的化合物其中R 1和R 2独立地表示氢,被1至4个碳原子的烷基取代的氨基甲酰基,2至5个碳原子的烷基羰基或苯基羰基,X表示卤素硝基或氰基, R 3表示其中R 4表示氰基或2至5个碳原子的烷基羰基,R 5表示未被取代或被1至8个碳原子的烷基或被1至8个碳原子的羟基烷基取代的氨基甲酰基或药学上可接受的酯 及其盐及其药学上可接受的载体,以及含有所述化合物作为COMT抑制剂的药物组合物。
摘要:
Pharmacologically active catechol derivatives of formula I ##STR1## wherein R.sub.1 and R.sub.2 independently comprise hydrogen, alkyl, acyl, optionally substituted aroyl, lower alkylsulfonyl or alkylcabamoyl or taken together form a lower alkylidene or cycloalkylidene, X comprises an electronegative substituent such as halogen, nitro, cyano, lower alkylsulfonyl, sulfonamido, aldehyde, caboxyl or trifluoromethyl and R.sub.3 comprises hydrogen, halogen, hydroxy alkyl, amino, nitro, cyano, trifluoromethyl, lower alkylsulfonyl, sulfonamide, aldehyde, alkyl carbonyl, aralkylidene carbonyl or carboxyl or a group selected from ##STR2## wherein R.sub.4 comprises hydrogen, alkyl, cyano, carboxyl or acyl and R.sub.5 comprises hydrogen, cyano, carboxyl, alkoxycarbonyl, carboxyalkenyl, nitro, acyl, optionally substituted aroyl or heteroaroyl, hydroxyalkyl or carboxyalkyl or R.sub.4 and R.sub.5 together form a five to seven membered substituted cycloalkanone ring;--(CO).sub.n (CH.sub.2).sub.m --CORwherein n is 0-1 and m is 0-7 and R comprises hydroxy, alkyl, carboxyalkyl, optionally substituted alkene, alkoxy or optionally substituted amino; ##STR3## wherein R.sub.8 and R.sub.9 independently comprise hydrogen or one of the following optionally substituted groups; alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, or together form an optionally substituted piperidyl group;--NH--CO--R.sub.10wherein R.sub.10 comprises a substituted alkyl group.
摘要:
A process for the preparation of nitrophenols by adding over a period of time a suspension containing from about 4 to about 20 per cent weight/volume of nitrosated phenol to a nitric acid solution containing between 45 and 100 per cent by weight of nitric acid, said solution being maintained at a temperature in the range from about 45.degree. to 100.degree.C.
摘要:
A PROCESS IS PROVIDED FOR MAKING 2,4-DI-NITRO-6-SECALKYLPHENOLS USING BOTH 2,6-DI-SEC-ALKYLPHENOLS AND OSEC-ALKYLPHENOLS AS STARTING MATERIAL. IN THE FIRST STEP, 2,6DI-SEC-ALKYLPHENOLS ARE ADDED TO EXCESS CONCENTRATED SULFURIC ACID AT 75-150*C. CAUSING CONCURRENT DEALKYLATION AND SULFONATION. IN THE SECOND STEP, O-SEC-ALKYLPHENOLS ARE ADDED TO CONSUME MOST OF THE REMAINING SULFURIC ACID, PERMITTING REPLACEMENT OF SULFONIC ACID GROUPS WITH NITRO GROUPS BY REACTING THE FINAL MIXTURE WITH AQUEOUS ALKALI METAL NITRATES. THE PRODUCTS (E.G., 2,4-DI-NITRO-6-SEC-BUTYLPHENOL) ARE USEFUL AS SELECTIVE HERBICIDES.