CAS: 674-26-0; 4-Hydroxy-4-Methyltetrahydro-2H-Pyran-2-One

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19115-49-2 53771-22-5 73834-54-5

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葡萄糖置于e.Coli-Se1体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 48.0H,反应生成 甲瓦龙酸内酯
参考文献:Processes For Conversion Of Biologically Derived Mevalonic Acid
标题:Processes For Conversion Of Biologically Derived Mevalonic Acid
摘要:这项发明涉及一种过程,包括将甲烷酸或含有甲烷酸的溶液反应,以产生第一产品或第一产品混合物,可选地在固体催化剂的存在下和/或在升高的温度和/或压力下.该发明还涉及一种过程,包括:(A)提供表达生物合成甲烷酸途径的微生物生物体;(B)在包含适当碳基底物的发酵培养基中培养微生物生物体,从而产生生物基甲烷酸;以及(C)将所述生物基甲烷酸反应,以产生第一产品或第一产品混合物.

专利信息

专利号:US-5118853-A
优先权日:1988-10-13
标题:Processes for the synthesis of 3-disubstituted aminoacroleins
发明人：LEE GEORGE T; REPIC OLJAN
权利人:SANDOZ LTD
摘要:Process for the synthesis of compounds of the formula ##STR1## comprising the steps of (i) reacting a compound of the formula ##STR2## with oxalyl chloride or oxalyl bromide to form the corresponding compound of the formula ##STR3## (ii) reacting said compound of the formula ##STR4## with a compound of the formula ##STR5## to form the corresponding compound of the formula ##STR6## (iii) hydrolyzing said compound of the formula ##STR7## to obtain the corresponding compound of the formula ##STR8## the use of the compounds of the formula ##STR9## for the synthesis of the compounds of the formula ##STR10## and the use of the intermediates of Formula VII for the direct synthesis of the compounds of Formula II, n wherein n R 1 is C 1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 1b is phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 2 is C 1-3 alkyl, n one of R 3 and R 4 is ##STR11## and the other is primary or secondary C 1-6 alkyl not containing an asymmetric carbon atom, C 3-6 cycloalkyl or phenyl-(CH 2 ) m -, n wherein n R 7 is hydrogen, C 1-3 alkyl, n-butyl, i-butyl, t-butyl, C 1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, n R 8 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, n R 9 is hydrogen, C 1-2 alkyl, C 1-2 alkoxy, fluoro or chloro, and n m is 1, 2 or 3, with the provisos that not more than one of R 7 and R 8 is trifluoromethyl, not more than one of R 7 and R 8 is phenoxy, and not more than one of R 7 and R 8 is benzyloxy, n R 5 is hydrogen, C 1-3 alkyl, n-butyl, i-butyl, t-butyl, C 3-6 cycloalkyl, C 1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, and n R 6 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy, or benzyloxy, with the provisos that not more than one of R 5 and R 6 is trifluoromethyl, not more than one of R 5 and R 6 is phenoxy, and not more than one of R 5 and R 6 is benzyloxy, n R 10 is C 1-6 alkyl, each X is chloro or bromo, and each X.sup.⊖ is chloride or bromide.

专利号:US-5290946-A
优先权日:1988-10-13
标 题 :Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes
发明人：LEE GEORGE T; KAPA PRASAD K; REPIC OLJAN
权利人:SANDOZ LTD
摘要:A process for synthesizing compounds of the formula ##STR1## utilizing, as intermediates, oxalyl chloride or bromide and compounds of the formulae R 1 R 2 N--CHO and CH 2 â•?CH--O--R 10 are processes for synthesizing compounds of the formula ##STR2## utilizing, as intermediates, compounds of Formula I wherein R 1 is phenyl or substituted phenyl or intermediates in the synthesis of the compounds of formula I which intermediates have the formula ##STR3## wherein R 1 is C 1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 2 is C 1-3 alkyl, n R 10 is C 1-6 alkyl, n X.sup.⊖ is chloride or bromide, and n R 3 -R 6 are as defined in the specification. n The compounds of Formula II are intermediates in the synthesis of known HMB-CoA reductase inhibitors which inhibit the biosynthesis of cholesterol and are useful as antihyperchloesterolemic gents.

专利号:US-4739073-A
优先权日:1983-11-04
标题:Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof
发明人：KATHAWALA FAIZULLA G
权利人:SANDOZ PHARMACEUTICALS CORP
摘要:Compounds of the formula wherein one of R and Ro is and the other is primary or secondary C1-6alkyl not containing an asymmetric carbon atom, C3-6cycloalkyl or phenyl(CH2)m-, wherein R4 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5a is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R5 and R5a must be hydrogen when R4 is hydrogen, R5a must be hydrogen when R5 is hydrogen, not more than one of R4 and R5 is trifluoromethyl, not more than one of R4 and R5 is phenoxy, and not more than one of R4 and R5 is benzyloxy, R2 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C3-6cycloalkyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R3 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R3 must be hydrogen when R2 is hydrogen, not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, and not more than one of R2 and R3 is benzyloxy, X is -(CH2)n- or -CH=CH-, wherein n is 0, 1, 2 or 3, and Z is wherein R6 is hydrogen or C1-3alkyl, and R7 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, benzyl or M, wherein M is a pharmaceutically acceptable cation, 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-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:WO-2014052054-A1
优先权日:2012-09-25
标题 :Enzymatic platform for the synthesis of isoprenoid precursors and uses thereof
发明人：LEYH THOMAS S
权利人:EINSTEIN COLL MED
摘要:Provided are method of synthesizing (R)-5-diphosphomevalonate (DPM), isopentenyl 5-pyrophosphase (IPP), dimethylallyl 5 -pyrophosphate (DMAPP) and isoprenoid using a one-pot synthesis.

专利号:US-4613610-A
优先权日:1984-06-22
标题 :Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives
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, each of R2 and R5 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenyl, phenoxy or benzyloxy, each of R3 and R6 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, each of R4 and R7 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, not more than one of R2 and R3 is benzyloxy, not more than one of R5 and R6 is trifluoromethyl, not more than one of R5 and R6 is phenoxy, and not more than one of R5 and R6 is benzyloxy, 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 R10 is hydrogen or C1-3alkyl, wherein R12 is a physiologically acceptable and hydrolyzable ester group, and M is a pharmaceutically acceptable cation, with the provisos that (i) the-X-Z group is in the 4- or 5-position of the pyrazole ring, and (ii) the R1 group and the -X-Z group are ortho to each other, 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.