36192-01-5Relevant articles and documents
Tasimelteon intermediate and preparation method thereof
-
Paragraph 0036-0039, (2017/04/27)
The invention provides a tasimelteon intermediate and a preparation method thereof. The preparation method comprises the following steps: with a compound a as a raw material, reacting the compound a with benzyl bromide so as to obtain a compound I; then subjecting the compound I to a reaction under the action of a combined catalyst consisting of potassium osmate dihydrate, potassium carbonate, potassium ferricyanide, benzyltriethylammonium chloride and methane sulfonamide or a combined catalyst consisting of osmium tetroxide, potassium carbonate, potassium ferricyanide, benzyltriethylammonium chloride and methane sulfonamide so as to obtain a compound II; subjecting the compound II to an oxidation reaction under the action of sodium periodate or lead tetraacetate so as to obtain an intermediate compound III and carrying out a reduction reaction so as to obtain a compound IV; and subjecting the compound IV to a reduction reaction to remove a benzyl protective group so as to obtain a compound V, then reacting the compound V with p-toluene sulfonyl chloride, carrying out hydroxyl protection and then carrying out cyclization under the action of potassium carbonate so as to obtain the tasimelteon intermediate compound VI. The invention provides a novel process for preparation of the tasimelteon intermediate; and the prepared tasimelteon intermediate has good purity and high quality and is applicable to industrial production.
Tricyclic tetrahydro naphthaleneols and related compounds
-
, (2008/06/13)
Compounds are provided of the structure STR1 WHEREIN X--Z--Y together with two carbons of the cycloalkyl ring form a 5- or 6-membered ring, wherein R1 is hydrogen, aralkyl or acyl, n is 0, 1 or 2, and n' is 0, 1, 2 or 3, R2 is hydrogen, lower alkyl or aralkyl, R3 is hydrogen, acyl, lower alkyl, aralkyl, lower alkoxy, carboxy, halo, alkenyl, nitro, cycloalkyl, amino, acylamino, R2 O(CH2)n 2 where n2 is 0, 1 or 2 or dihydroxyalkyl, X and Y may be the same or different and can be --CH2 --, =N--, --O--, --S--, --NR4 --, --O--CH2 --, --S--CH2 --, or --NR4 --CH2 -- where R4 is hydrogen, lower alkyl or aryl, Z can be STR2 where R5 and R6 can be hydrogen, lower alkyl, cycloalkyl, aryl, haloalkyl, amino or substituted or unsubstituted aminoalkyl; STR3 and --X--Z--Y-- can be taken together to form STR4 and STR5 These compounds are useful as anti-fibrillatory agents, disinfectants and water-softeners.
2,3-Trans-5-[3-(amino)-2-hydroxy-propoxy]-1,2,3,4-tetrahydro-3-(or 2)-amino-2-(or 3)-hydroxy-naphthalenes and salts thereof
-
, (2008/06/13)
This invention relates to novel cyclic polymethylene phenoxy-aminopropanols having the structure STR1 and the pharmaceutically acceptable salts of said compounds, wherein R1, R2, R8 and R9 are each independently selected from hydrogen, lower alkyl and aryl-lower alkyl and R3, R4, R5, R6 and R7 are each independently selected from hydrogen and lower alkyl, which are useful in the treatment of coronary diseases.
Naphthyloxy acetic acids and related compounds
-
, (2008/06/13)
Compounds are provided having the structure: SPC1 And to salts of such compounds. These compounds are useful as hypocholesteremic agents and anti-inflammatory agents.