Abstract:
Process for the preparation of compounds (I), wherein A and R are defined as in Claim 1, by reaction of phenyl-glycine (VII) in the presence of alkanol with 1.05-1.3 moles of alkali hydroxide and reacting the mixture with an acid with a higher pH value than 4.3, or by reaction of (VII) with an equivalent amount of alkali salts of acids possessing a higher pH value than 4.3, and condensing the obtained amino acid salt in the presence of alkanol with a compound (VIII) -R is defined as in Claim 1- at the boiling point of the reaction mixture, removing water continuously from the reaction mixture by a binary or ternary azeotropic distillation. The thus obtained compound is optionally reacted with a reactive trifluoro-methane sulphonic acid derivative.
Abstract:
The invention relates to an improved, large scale process for the preparation of compounds of formula (I), wherein R is halogen atom or hydroxyl, R is hydrogen atom or hydroxyl, R and R are hydrogen or alkoxy having 1-6 carbon atoms.
Abstract:
The invention relates to an improved process for preparing amidoxime derivatives of general formula (I), wherein R means a C2-15 group, which may be unsaturated and/or cyclic alkyl, aralkyl group or optionally substituted and/or condensed aromatic and/or heteroaromatic group; R stands for hydrogen or an optionally substituted straight or branched chain or cyclic and/or unsaturated C1-7 alkyl or aromatic group; R represents an optionally substituted straight or branched chain or cylic and/or unsaturated C1-7 alkyl or aromatic group; or R and R together with the adjacent nitrogen atom may form a 5- to 8-membered ring optionally containing other heteroatom(s); and X stands for halogen and their salts by reacting an amidoxime of general formula (II), wherein R is as defined above, in the presence of an alkaline substance, transforming the product to a salt with an acid or transforming the salt to the base, which comprises reacting the amidoxime with an alkaline metal hydroxide or alkaline metal alkoxide and dimethylformamide or 1,3-dimethyl-2-imidazolidinone, preferably in the presence of a proton source, reacting the amidoxime complex thus obtained preferably without isolation with an amine of general formula (III). The invention relates further to pure O-(2-hydroxy-piperidino-1-propil)nicotinic acid amidoxime hydrochloride and hydrobromide and O-(2-hydroxy-3-piperidino-1-propyl)nicotinic acid amidoxime base.
Abstract translation:本发明涉及一种制备通式(I)的偕胺肟衍生物的改进方法,其中R 1表示C2-15基团,其可以是不饱和和/或环状烷基,芳烷基或任选取代的和/或稠合的芳族 和/或杂芳族基团; R 2代表氢或任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; R 3表示任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; 或R 2和R 3与相邻的氮原子一起可以形成任选含有其它杂原子的5-至8-元环; X代表卤素及其盐,通过在碱存在下使通式(II)的偕胺肟(其中R 1如上述定义)在酸存在下反应,将产物转化为酸或转化盐 包括使偕胺肟与碱金属氢氧化物或碱金属醇盐和二甲基甲酰胺或1,3-二甲基-2-咪唑啉酮反应,优选在质子源存在下,使得到的偕胺肟配合物优选不与其分离而与 通式(III)的胺。 本发明还涉及纯O-(2-羟基 - 哌啶子基-1-丙基)烟酸偕胺肟盐酸盐和氢溴酸盐和O-(2-羟基-3-哌啶子基-1-丙基)烟酸偕胺肟碱。
Abstract:
New N-[2-(4-fluoro-phenyl)-1-methyl]-ethyl-N-methyl-N-propynyl amine of the general formula (I), and isomers and salts thereof. The compound of the formula (I) is useful as medicine. The compound of the formula (I), may be prepared by methods known per se.
Abstract:
Process for the preparation of compounds (I), wherein X, Y, A and R are defined as in Claim 1, by reaction of a substituted phenyl-glycine (VII) in the presence of alkanol with 1.05-1.3 moles of alkali-hydroxide and reacting the reaction mixture with an acid, the pH-value of which is higher than 4.3, or by reaction of (VII) with an equivalent amount of alkali salts derived from acids having a pH value higher than 4.3, and condensing the obtained amine acid salt in the presence of alkanol with a compound (VIII) -R is defined as in Claim 1- at the boiling point of the reaction mixture, removing water continuously from the reaction mixture by a binary or ternary azeotropic distillation. The thus obtained compound is optionally reacted with a reactive derivative of trifluoro-methane-sulphonic acid.
Abstract:
The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives. The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide. The combinations according to the invention bear an outstanding importance in the protection of stored crops.
Abstract:
The invention relates to a process for the preparation of such isomer mixtures of cypermethrine of formula (I), wherein carbon atoms indicated by 1,3 and α stand for a chiral carbon atom and the wavy line indicates cis or trans configuration related to the cyclopropane ring - which contains out of the theoretically possible 8-isomers of cypermethrine at least 95 % of 1RtransS and 1StransR (Ib) isomer pair or only a mixture of 1RcisS and 1ScisR (Ia) and the isomer pair (Ib) of the ratio (Ia):(Ib) = 55:45 - 25:75 by asymmetric transformation of second order performed in the presence of an amine base and solvent from a starting cypermethrine isomer mixture which contains next to the isomer pair (Ib) cis and other trans isomers or the isomer pair Ia + Ib at an undesired ratio.
Abstract:
The compounds of general Formula I (wherein R is hydrogen or halogen) and pharmaceutically acceptable acid addition salts thereof are suitable for the prophylaxis of undesired and unfavourable symptoms (e.g. perspiration, nausea, vomiting, dizziness, etc.)which occur when healthy humans or mammal animals are subjected to unusual moving (e.g. during transportation on aeroplane, or vehicles, ships, etc.). The invention relates to the above pharmaceutical compositions and a process for the preparation thereof.
Abstract:
A process for the preparation of decolourized products containing formed elements of blood such as full blood powder, hemoglobin powder, blood concentrates and processes to prepare food additives and foods of the same, from solutions, suspensions or emulsions containing formed elements of blood, by adding anticoagulants, opening the formed elements of blood containing hemoglobin by known methods, and if desired concentrating the compositions thus obtained and/or freeze drying the same. The invention is performed by adjusting the pH value of the mixture containing the open formed elements and the hemoglobin to pH = 1-2, treating the mixture with an oxidizing agent in the presence of a carbohydrate derivative containing a dienol-group, if desired dialyzing the solution thus obtained to eliminate the by-products, concentrating the solution until a dry substance content of 10-40 % w/v is obtained before or after adjusting the pH value to 7-7.5 and - if desired - freeze drying the product.