摘要:
A process for the preparation of C.sub.14 -C.sub.18 -alkylphosphocholines by reacting an n-alkanol with a chain length of C.sub.14 -C.sub.18 with phosphorus oxychloride in an inert solvent or also without solvent in the presence or absence of a basic substance in a single vessel process and subsequent reaction of the reaction product in an inert solvent with a choline salt in the presence of a basic substance to form phosphoric acid diester chloride, subsequent hydrolysis and isolation of alkylphosphocholine as well as optionally purification using a mixed-bed ion exchanger or in successive steps with an acid ion exchanger and a basic ion exchanger.
摘要:
A process for the preparation of C.sub.14 -C.sub.18 -alkylphosphocholines by reacting an n-alkanol with a chain length of C.sub.14 -C.sub.18 with phosphorus oxychloride in an inert solvent or also without solvent in the presence or absence of a basic substance in a single vessel process and subsequent reaction of the reaction product in an inert solvent with a choline salt in the presence of a basic substance to form phosphoric acid diester chloride, subsequent hydrolysis and isolation of alkylphosphocholine as well as optionally purification using a mixed-bed ion exchanger or in successive steps with an acid ion exchanger and a basic ion exchanger.
摘要:
This disclosure describes two technical procedures for the high-yield synthesis of heterocyclic seven-membered ring-systems by Dieckmann-condensation avoiding usual dilution techniques and long reaction times. Thus, it significantly increases the overall yields of the pharmaceutically active ingredients azelastine and flezelastine, whose synthesis, starting from these seven-membered heterocyclic rings, is reported elsewhere. Yields range from 80-89%, avoiding waste and increasing economics of the synthesis.
摘要:
The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which at least one of the groups Z1, Z2, Z3 is selected from —O—, —S—, —NH—, —N(—CH3)—, whereas the other groups Z1, Z2, Z3 have the meaning of a —CH2— group, and in which Ar is an aromatic group.
摘要:
The invention relates to novel modifications of the compound 2-amino-4-(4-fluorobenzylamino)-1-ethoxy-carbonylaminobenzene of the processes for their preparation and their use in pharmaceutical compositions.
摘要:
A method for synthesising a compound having the general formula (I) wherein R represents substituents selected independently from the group of H, F, Cl, Br, NO2, alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy and disubstituted amine R′ is independently selected from the group of H, F, Cl, Br, OH, NO2, alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy and disubstituted amine, n is selected from 1, 2 or 3.
摘要:
Tripeptide boronic acids of (R,S,R) configuration, for example Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2, and their use to make base addition salts of such acids. The salts are formulated into anti-thrombotic pharmaceutical formulations.
摘要:
The invention relates to the production and purification of salts of 6,8-bis (amidiniumthio)octanoic acid, its enantiomers (+)-6,8-bis(amidiniumthio)octanoic acid and (-)-6,8-bis (amidiniumthio)octanoic acid and of the esters of these compounds as well as to their use to produce dihydrolipoic acid and .alpha.-lipoic acid.
摘要:
Organoboronic acids, for example Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2, are made by hydrolysing their diethanolamine adducts under conditions which avoid substantial C—B bond breakage. The product acids are substantially free of degradation product derived from cleavage of the C—B bond thereof. The acids are used to make base addition salts thereof. The salts are formulated into anti-thrombotic pharmaceutical formulations.
摘要:
A process for preparation of pure flupertine maleate and the pure A crystalline form of flupertine maleate by the use of water soluble alcohols during synthesis and/or purification.