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CAS号2983-26-8 1,2-二溴乙氧基乙烷 | CAS号109-92-2 乙烯基乙醚 | CAS号761-17-1 DIBROMOACETALDE... | CAS号77295-79-5 2-ethoxy-1,1-di... | CAS号768-95-6 1-金刚烷醇 | CAS号75-65-0 叔丁醇 | CAS号927-80-0 乙氧基乙炔,己烷溶液 | CAS号112-31-2 癸醛 | CAS号64724-29-4 三丁基(2-乙氧基乙烯基)锡 | CAS号22411-59-2 反式4-(二乙氨基)肉桂醛 | CAS号64724-28-3 lithium,ethenox... | CAS号60036-64-8 (Z)-3-ethoxyacr... | CAS号58243-08-6 反式-3-乙氧基丙烯腈 | CAS号5623-82-5 2-cyclopentylid...合成工艺路线路线简述
- 合成目标产物 Cis-1-Bromo-2-Ethoxyethylene 主要起始原料 Ethyl Vinyl Ether
- (文献来源)合成步骤主要原料 Ethyl Vinyl Ether
📜1,1-二溴-2,2-二乙氧基乙烷置于甲烷体系中,化学反应生成顺-1-溴-2-乙氧基乙烯
参考文献:Jp158
标题:Jp158
专利信息
专利号:US-4973704-A
优先权日:1985-10-25
标题 :Pyrrolyl intermediates in the synthesis of pyrrole analogs of mevalonolactone and derivatives thereof
发明人:WAREING JAMES R
权利人:SANDOZ PHARMACEUTICALS CORP
摘要:Compounds of the formula wherein R1 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R5, R6 and R7 are as defined below, R2 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R8, R9 and R10 are as defined below, R3 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R11, R12 and R13 are as defined below, R4 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R14, R15 and R16 are as defined below, X is -(CH2)m-, -CH=CH-, -CH=CH-CH2-or -CH2-CH=CH-, wherein m is 0, 1, 2 or 3, and Z is wherein R17 is hydrogen or C1-3alkyl, and R18 is hydrogen, R19 or M, wherein R19 is a physiologically acceptable ester group, and M is a pharmaceutically acceptable cation, wherein each of R5, R8, R11 and R14 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy, each of R6, R9, R12 and R15 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, and each of R7, R10, R13 and R16 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one substituent on each of Rings A, B, C and D independently is trifluoromethyl, not more than one substituent on each of Rings A, B, C and D independently is phenoxy, and not more than one substituent on each of Rings A, B, C and D independently is benzyloxy, with the provisos that (i) the -X-Z group is in the 2- or 3-position of the pyrrole ring, (ii) the -X-Z group is ortho to both R1 and R2 and (iii) R3 is ortho to R2, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-4851427-A
优先权日:1985-10-25
标 题 :Pyrrole analogs of mevalonolactone, derivatives thereof and pharmaceutical use
发明人:WAREING JAMES R
权利人:SANDOZ PHARMACEUTICALS CORP
摘要:Compounds of the formula wherein R1 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R5, R6 and R7 are as defined below, R2 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R8, R9 and R10 are as defined below. R3 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R11, R12 and R13 are as defined below, R4 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C7-7cycloalkyl or wherein R14, R15 and R16 are as defined below, X is -(CH2)m-, -CH=CH-, -CH=CH-CH2- or -CH2-CH=CH-, wherein m is 0, 1, 2 or 3, and Z is wherein R17 is hydrogen or C1-3alkyl, and R18 is hydrogen, R19 or M, wherein R19 is a physiologically acceptable ester group, and M is a pharmaceutically acceptable cation, wherein each of R5, R8, R11 and R14 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy, each of R6, R9, R12 and R15 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, and each of R7, R10, R13 and R16 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one substituent on each of Rings A, B, C and D independently is trifluoromethyl, not more than one substituent on each of Rings A, B, C and D independently is phenoxy, and not more than one substituent on each of Rings A, B, C and D independently is benzyloxy, with the provisos that (i) the -X-Z group is in the 2- or 3-position of the pyrrole ring, (ii) the -X-Z group is ortho to both R1 and R2, and (iii) R3 is ortho to R2, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-7067703-B2
优先权日:2001-10-31
标题:Manufacture of retinoids
发明人:RADSPIELER ALEXANDER; RUETTIMANN AUGUST
权利人:DSM IP ASSETS BV
摘要:A process for the manufacture of retinal (I) comprises reacting a 5-(2,6,6-trimethyl-cyclohex-1-enyl)-1,4-pentadiene derivative (IIa) or a 5-(2,6,6-trimethyl-cyclohex-2-enyl)-1,4-pentadiene derivative (IIb) or a 5-(2,6,6-trimethyl-2-cyclohexen-1-ylidene)-1-pentene derivative (IIc) or a 5-(2,6,6-trimethyl-cyclohex-1-enyl)-penta-1-en-4-yne derivative (IId) or a 5-(2,6,6-trimethyl-cyclohex-2-enyl)-penta-1-en-4-yne derivative (IIe) with a 1,3-butadiene derivative H2Câ•?C(CH3)CCHâ•?CHOR4 (III) in the presence of a Lewis or Brönsted acid and subjecting the compound obtained in each case [(IVa), (IVb), (IVc), (IVd) or (IVe), respectively] to basic or acidic conditions to eliminate therefrom the moiety R2H and thus produce, according to the immediate precursor, retinal itself or a particular derivative thereof [(I′), (I″), (Va) or (Vb), respectively] and, where in two cases such derivative is produced featuring a triple bond [derivative (Va) or (Vb)], hydrogenating this to produce retinal (I) or the derivative (I′), respectively, and each case where a derivative (I′) or (I″) has been produced, isomerizing this under basic or acidic conditions or in the presence of a metal catalyst to the desired retinal (I). The so-produced retinal is usually in the form of an isomeric mixture, normally as (9 E/Z, 13 E/Z)-retinal, and this can be isomerized according to a further inventive aspect to (all-E)-retinal by the acid-catalyzed formation of an adduct of (all-E)-retinal with hydroquinone in crystalline form. The so obtained (all-E)-retinal-hydroquinone adduct can then if desired be converted to vitamin A alcohol in the predominantly (all-E)-isomeric form by a method known per se. The novel starting materials (IIa), (IIb), (IIc), (IVI) and (IIe) represent a still further inventive aspect. Retinal is a valuable intermediate in the synthesis of further vitamin A compounds (retinoids). The retinoids, particularly vitamin A alcohol (retinol), are known to be valuable substances which promote the well-being of humans, inter alia in respect of vision, the immune system and growth, and for this reason are often used as components of multivitamin preparations and as additives for crtain food- and feedstuffs.
专利号:US-8518952-B2
优先权日:2008-08-06
标题 :6 substituted 2-heterocyclylamino pyrazine compounds as CHK-1 inhibitors
发明人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER
权利人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER; PFIZER
摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.