欧盟法规
ECHA物质ECHA物质C&L通报REACH预注册专利信息
专利号:US-4459420-A
优先权日:1982-05-17
标题 :Pyrogallol synthesis of anti-atherogenic furochromones
发明人:GAMMILL RONALD B
权利人:UPJOHN CO
摘要:The present invention provides a total synthesis of known intermediates useful in the synthesis of khellin and antiatherosclerotic analogs thereof from pyrogallol. Pyrogallol is converted to 3,6,7-benzofurantriol triacetate using zinc chloride and chloracetanitrile, then catalytically reduced and deactoxylated at the 3 position to yield the corresponding 2,3-dihydrofuran. This substance is subjected to a Fries rearrangement to the corresponding diol, the phenolic hydroxyl group of which is then selectively alkylated. This yields 6-hydroxy-7-alkoxy-5-benzofuranyl methyl ketone, a known intermediate for the production of 4-desmethoxy khellin and analogs thereof. This compound is then selectively alkoxylated at the 4 position using lead tetraacetate or thallium (III) nitrate in an alkanol solvent to yield known chemical intermediates in the preparation of khellin and analogs thereof.
专利号:US-4384998-A
优先权日:1981-03-30
标题:Synthesis of thienamycin from D-glucose
发明人:DURETTE PHILIPPE L
权利人:MERCK & CO INC
摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-4448976-A
优先权日:1981-03-30
标题 :Chiral synthesis of thienamycin from D-gluocose
发明人:DURETTE PHILIPPE L
权利人:MERCK & CO INC
摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-4544502-A
优先权日:1981-03-30
标 题 :Chiral synthesis of thienamycin from D-glucose
发明人:DURETTE PHILIPPE L
权利人:MERCK & CO INC
摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-7897638-B2
优先权日:2005-04-12
标题:Synthesis of nitrodibenzylfuran chromophore for photodeprotection of organic molecules
发明人:ELLIS-DAVIES GRAHAM; MOMOTAKE ATSUYA
权利人:PHILADELPHIA HEALTH & EDUCATIO
摘要:Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).
专利号:US-4309346-A
优先权日:1980-03-27
标 题:Process for the preparation of 1-carbapenems and intermediates via trithioorthoacetates
发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N
权利人:MERCK & CO INC
摘要:Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via intermediates II and III: I II III wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R6 and R7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R1' is hydrogen or a protecting group; and Ra, Rb and Rc are independently selected from alkyl, aryl and aralkyl.