摘要:
Organic compounds containing a mercapto group or a dithiane moiety can be transformed into the analogous fluoro or difluoro compounds by reacting them with a halogenating reagent in liquid hydrogen fluoride, optionally containing boron trifluoride or antimony pentafluoride solution, at temperatures from about -80.degree. and 15.degree. C. The method may be descriptively termed "fluorodesulfurization".
摘要:
DL-Alanine, 3-fluoro-DL-alanine and 2-deutero-3-fluoro-DL-alanine, are resolved by reaction with a resolving base and a .beta.-dicarbonyl compound. The resulting azomethine diastereomeric salts which are easily separated, the masking group is readily removed under mildly acidic conditions.
摘要:
Described are 3-halovinylglycines and their amino acid dipeptide and oligopeptide conjugates, a new class of efficient antibacterial agents, pharmaceutical compositions containing them as active ingredients, and methods of synthesis. The compounds are thought to interfere in bacterial cell wall synthesis.
摘要:
Novel fluorinated diamine derivatives are inhibitors of ornithine decarboxylase enzyme and have the following general Formula I: ##STR1## wherein: R.sub.c represents hydrogen or carboxy;R.sub.1 represents hydrogen or C.sub.1 -C.sub.6 alkyl;Z represents methylene or oxygen;m and n each represent 0 or 1 but m+n=1; andp represents 1 or 2.
摘要翻译:新的氟化二胺衍生物是鸟氨酸脱羧酶的抑制剂,并具有以下通式I:其中:R c表示氢或羧基; R1代表氢或C1-C6烷基; Z表示亚甲基或氧; m和n各自表示0或1,但m + n = 1; p表示1或2。
摘要:
There is provided, a novel class of compounds exhibiting antibacterial activity, said compounds having the formula: ##EQU1## wherein X and Y each represent a member which may be the same or different selected from the group consisting of H and Cl with the priviso that X and Y cannot represent H simultaneously; R.sub.1 and R.sub.2 each represent a member which may be the same or different selected from the group consisting of an n- or branched alkyl group of from 1 to 20 carbon atoms, an aryl group (phenyl, naphthyl, etc.) and a ##EQU2## (CH.sub.2).sub.n group, wherein n represents an integer of from 2 - 5; and Z represents a member selected from the group consisting of an --OR.sub.3 group, a a ##EQU3## wherein R.sub.4 and R.sub.5 each represent a member which may be the same or different selected from the group consisting of H and an alkyl group of from 1 - 3 carbon atoms, wherein R.sub.6 and R.sub.7 each represent a member which may be the same or different selected from the group consisting of R.sub.1, R.sub.2, or H when X is not Cl or R.sub.1 and R.sub.2 when X is Cl, wherein R.sub.1 and R.sub.2 are defined above, wherein X is as defined above, and wherein R.sub.3 in each case represents a member selected from the group consisting of an n- or branched alkyl group of from 2 - 20 carbon atoms, a --OCH.sub.2 CH.sub.2 (OCH.sub.2 CH.sub.2).sub.n --OR.sub.1 group, wherein R.sub.1 is defined as above and n represents an integer of from 1 - 11, aGroup, wherein W represents a member selected from the group consisting of H, an n- or branched alkyl group of from 1 - 20 carbon atoms, a halogen atom, (Cl, Br, I), an --OR.sub.8 group, and a ##EQU4## group, wherein R.sub.4 and R.sub.5 are as defined above and R.sub.8 represents a member selcted from the group consisting of H and R.sub.1, wherein R.sub.1 is as defined above, and --CH.sub.2 CH.sub.2 --(OCH.sub.2 CH.sub.2).sub.n -- ##SPC1##Group, wherein n represens an integer of from 1 - 20 and R.sub.1 is as defined above,With the further proviso that when X and Y are Cl and R.sub.1 and R.sub.2 are methyl, Z cannot be a member selected from the group consisting of --OCH.sub.3 and NH.sub.2.
摘要:
POLYFLUOROISOALKOXYALKYL AMIDO CARBOXYLIC ACIDS OF THE FORMULA:
R1-CF(-R2)-CF(-CF(-R3)-R4)-O-R-CO-N(-R5)-R6-COOH
WHEREIN R1-R4 ARE EACH INDEPENDENTLY SELECTED FROM THE GROUP CONSISTING OF F, CL, ALKYL AND HALOALKYL GROUPS IN WHICH THE HALOGEN ATOMS ARE CL OR F; R1 AND R4 WHEN TAKEN TOGETHER ARE ALKYLENE OR HALOALKYLENE GROUPS WHICH FORM, WITH THE CARBON CHAIN THEREBETWEEN, A CYCLIC STRUCTURE; R IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF ALKYLENE AND HALOALKYLENE; R5 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKYL, AND R6 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF ALKYLENE, MONOHYDROXYALKYLENE AND CARBOXYALKYLENE RADICALS; AND SALTS THEREOF CONTAINING A CATION SELECTED FROM THE GROUP CONSISTING OF LI, NA, K, RB, CS, CA, BA, MG, ZN, HG, AL, CR, SN, FE, AG, CU, CO, ZR, PB, MN, OR A RADICAL SELECTED FROM MORPHOLINO, AMMONIUM OR AN ALKYL OR HYDROXYALKYL SUBSTITUTED AMMONIUM RADICAL. PREPARATION BY REACTING CORRESPONDING POLYFLUOROISOALKOXYALKYL AMIDO CARBOXYLIC ACID FLUORIDES OR HALOSULFATES WITH AMINO ACIDS. THE NOVEL COMPOUNDS ARE USEFUL AS EMULSIFYING AGENTS, LEVELING AGENTS, OIL, STAIN AND WATER REPELLENT AGENTS, ADDITIVES TO DRY POWDER FIRE EXTINGUSHING COMPOSITIONS AND AS INTERMEDIATES TO VALUABLE OIL, STAIN AND WATER REPELLENT AGENTS.
摘要:
The N-methyl-D-glucamine salt of (+)-2-(2-fluoro-4-biphenylyl)propionic acid, which is a novel compound with analgesic, anti-inflammatory and antipyretic properties and which is useful for treating inflammatory conditions including rheumatic disorders and as an analgesic. Pharmaceutical compositions containing the novel salt are also described. Also described are methods for preparing the novel salt by direct salification in an aqueous or non-aqueous medium, for example isopropanol, aqueous tetrahydrofuran, bis(methoxyethyl) ether and 4-methyl-1,3-dioxolan-2-one. Isopropanol is especially preferred.