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1. 发明授权

US5118853A Processes for the synthesis of 3-disubstituted aminoacroleins 失效
公开(公告)号：US5118853A
公开(公告)日：1992-06-02
申请号：US661286
申请日：1991-02-26
申请人： George T. Lee , Oljan Repic
发明人： George T. Lee , Oljan Repic
IPC分类号： C07C51/367 , C07D209/12 , C07D209/24 , C07D233/54
CPC分类号： C07D233/64 , C07C51/367 , C07D209/12 , C07D209/24
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,whereinR.sub.1 is C.sub.1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups),R.sub.1b is phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups),R.sub.2 is C.sub.1-3 alkyl,one of R.sub.3 and R.sub.4 is ##STR11## and the other is primary or secondary C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-6 cycloalkyl or phenyl-(CH.sub.2).sub.m -,whereinR.sub.7 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.8 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.9 is hydrogen, C.sub.1-2 alkyl, C.sub.1-2 alkoxy, fluoro or chloro, andm is 1, 2 or 3, with the provisos that not more than one of R.sub.7 and R.sub.8 is trifluoromethyl, not more than one of R.sub.7 and R.sub.8 is phenoxy, and not more than one of R.sub.7 and R.sub.8 is benzyloxy,R.sub.5 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.3-6 cycloalkyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, andR.sub.6 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy, or benzyloxy, with the provisos that not more than one of R.sub.5 and R.sub.6 is trifluoromethyl, not more than one of R.sub.5 and R.sub.6 is phenoxy, and not more than one of R.sub.5 and R.sub.6 is benzyloxy,R.sub.10 is C.sub.1-6 alkyl, each X is chloro or bromo, and each X.sup..crclbar. is chloride or bromide.

2. 发明授权

US5290946A Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes 失效
标题翻译：用于合成3-（取代的吲哚基-2-基）丙醛的方法
公开(公告)号：US5290946A
公开(公告)日：1994-03-01
申请号：US980055
申请日：1992-11-23
申请人： George T. Lee , Prasad K. Kapa , Oljan Repic
发明人： George T. Lee , Prasad K. Kapa , Oljan Repic
IPC分类号： C07C51/367 , C07C59/48 , C07C223/02 , C07D209/12 , C07D209/24 , C07D233/54
CPC分类号： C07D233/64 , C07C223/02 , C07C51/367 , C07C59/48 , C07D209/12 , C07D209/24
摘要： A process for synthesizing compounds of the formula ##STR1## utilizing, as intermediates, oxalyl chloride or bromide and compounds of the formulae R.sub.1 R.sub.2 N--CHO and CH.sub.2 .dbd.CH--O--R.sub.10 are processes for synthesizing compounds of the formula ##STR2## utilizing, as intermediates, compounds of Formula I wherein R.sub.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.sub.1 is C.sub.1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups),R.sub.2 is C.sub.1-3 alkyl,R.sub.10 is C.sub.1-6 alkyl,X.sup..crclbar. is chloride or bromide, andR.sub.3 -R.sub.6 are as defined in the specification.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 agents.
摘要翻译：合成式（I）化合物的方法利用草酰氯或溴化物作为中间体，式R1R2N-CHO和CH2 = CH-O-R10的化合物是合成下式化合物的方法：（II）使用式I化合物，其中R 1是苯基或取代的苯基或中间体在合成式I化合物中的中间体具有下式其中R 1是C 1-3烷基，苯基或苯基取代 1至3个取代基，各自独立地为C 1-3烷基，C 1-3烷氧基，氟，氯，溴或硝基（最多为两个硝基），R 2为C 1-3烷基，R 10为C 1-6烷基，X（ - ）为氯化物或溴化物，和R3-R6如说明书中所定义。式II化合物是合成已知的抑制胆固醇生物合成的HMB-CoA还原酶抑制剂的中间体，可用作抗高胆固醇酯剂。

3. 发明授权

US4318713A Method for gasifying cellulosic material 失效
标题翻译：气化纤维素材料的方法
公开(公告)号：US4318713A
公开(公告)日：1982-03-09
申请号：US192894
申请日：1980-10-01
申请人： George T. Lee , John N. Lees, Jr. , Paul M. Pukita
发明人： George T. Lee , John N. Lees, Jr. , Paul M. Pukita
IPC分类号： C10J3/06 , C10J3/00
CPC分类号： C10J3/005 , C10J3/06 , C10J3/723 , C10J3/74 , C10J2300/092 , C10J2300/0956 , C10J2300/0976
摘要： Method for gasifying cellulosic material comprises feeding cellulosic material into the uphill end of an inclined rotary kiln; transporting a bed of cellulosic material through the kiln and continuously tumbling the bed; withdrawing fuel gas from the uphill end of the kiln so it flows countercurrent to the bed and removes moisture in the drying zone and thermally decompose volatiles in the devolatilization zone; admitting air overbed in the devolatilization zone and only underbed in the gasifying zone; and controlling the mass flow rate of air into the devolatilization and gasifying zones respectively as predetermined percentages of that rate of which is stoichiometric to the cellulosic material fed into the kiln to thereby limit temperature rise, prevent agglomeration and minimize entrainment of solid particles. Air is admitted into the gasifying zone underbed through axially spaced sets of shell ports, and the mass flow rates of air therethrough are regulated as a function of the percentages of carbon in the bed in the portions of the kiln in which the sets of shell ports are disposed to thereby efficiently utilize the air in converting carbon into CO.sub.2, assure that a high percentage of CO.sub.2 is converted into chemical energy in the form of CO, and permit shortening of the kiln.
摘要翻译：气化纤维素材料的方法包括将纤维素材料进料到倾斜回转窑的上坡端; 运送纤维素材料床通过窑，并持续翻滚床; 从窑的上坡端取出燃料气体，使其与床层逆流流动，去除干燥区内的水分，并使脱挥发区内的挥发物热分解; 允许在脱挥发区内覆盖空气，仅在气化区进行铺层; 并分别控制进入脱挥发分气化区的空气的质量流量，其速率的预定百分比是与进料到窑中的纤维素材料的化学计量比，从而限制温度升高，防止团聚和最小化固体颗粒的夹带。空气进入气化区，通过轴向间隔开的一组壳体端口被层压，并且通过其中的空气的质量流率作为在窑的部分中的碳的百分比的函数来调节，其中壳体端口以便有效地利用空气将碳转化成二氧化碳，确保高比例的CO 2以CO的形式转化为化学能，并允许窑的缩短。

4. 发明授权

US5319123A Process for preparing substituted N-oxy-imidic acid derivatives 失效
标题翻译：制备取代的N-氧代亚氨基酸衍生物的方法
公开(公告)号：US5319123A
公开(公告)日：1994-06-07
申请号：US701933
申请日：1991-05-17
申请人： George T. Lee , Ustun B. Sunay , Prasad K. Kapa
发明人： George T. Lee , Ustun B. Sunay , Prasad K. Kapa
IPC分类号： C07C259/06 , C07C259/10 , C07C249/00
CPC分类号： C07C259/06 , C07C259/10 , Y02P20/55
摘要： N-oxy substituted imidic acid derivative of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are alkyl and aryl substituents, which are useful as antidiabetic and hypolipidemic agents are prepared by the following procedure: ##STR2## where X is chlorine, bromine, or iodine, and R.sub.1 ' is the same as R.sub.1 but with any hydroxy or carboxy groups present protected by a hydroxy or carboxy protecting group and, when R.sub.1 ' is a protected hydroxy or carboxy substituent, deprotecting the substituent.
摘要翻译：其中R 1，R 2和R 3是烷基和芳基取代基的N-氧取代的亚氨基酸衍生物，其用作抗糖尿病和降血脂剂是通过以下方法制备的：其中X是氯，溴，或碘，并且R 1'与R 1相同，但具有由羟基或羧基保护基团保护的任何羟基或羧基，并且当R 1'为被保护的羟基或羧基取代基时，使取代基脱保护。

5. 发明授权

US5608061A Process for preparing 1,4,8,11-tetraazacyclotetradecane 失效
标题翻译：制备1,4,8,11-四氮杂环十四烷的方法
公开(公告)号：US5608061A
公开(公告)日：1997-03-04
申请号：US510207
申请日：1995-08-02
申请人： Lech Ciszewski , John Amedio , Prasad Kapa , Andrew Kucerovy , George T. Lee
发明人： Lech Ciszewski , John Amedio , Prasad Kapa , Andrew Kucerovy , George T. Lee
IPC分类号： C07D257/02 , C07D255/02
CPC分类号： C07D257/02
摘要： An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the tetratosylation of an acyclic tetraamine to obtain a tetratoluenesulfonamide compound in a first step, the cyclization of said sulfonamide compound to obtain tetratosyl cyclam in a second step, and the detosylation of tetratosyl cyclam in a third step followed by basification to obtain the desired 1,4,8,11-tetraazacyclotetradecane.
摘要翻译：一种制备1,4,8,11-四氮杂环十四烷的改进方法，其包括无环四胺的四甲硅烷基化以在第一步中获得四磺酰胺化合物，在第二步中环化所述磺酰胺化合物以获得四基体环已烷，并进行脱甲苯基化在第三步骤中进行四糖基环化，然后碱化以获得所需的1,4,8,11-四氮杂环十四烷。

6. 发明授权

US4870199A Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 失效
标题翻译：合成二保护R [R *，S *] - 3,5-二羟基-6-氧代己酸酯的方法
公开(公告)号：US4870199A
公开(公告)日：1989-09-26
申请号：US166594
申请日：1988-03-10
申请人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
发明人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
IPC分类号： C07D209/18 , C07D233/54 , C07F7/18
CPC分类号： C07D233/64 , C07D209/18 , C07F7/1852 , Y02P20/55
摘要： Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, andR.sub.2z is C.sub.1-4 alkyl, benzyl or allyl,comprising, as a key step when R.sub.2z is R.sub.2x, the reaction of the compound of the formula ##STR2## in (S) enantiomeric form with a compound of the formulaMg.sup. .circle.+2 (.sup..crclbar. OOC--CH.sub.2 --COOR.sub.2x).sub.2to obtain a compound of the formula ##STR3## in (S) enantiomeric form, and, as a key step when R.sub.2z is R.sub.2y, the reaction of a compound of the formula ##STR4## in (S) enantioimeric form with a compound of the formulaLi.sup..sym..crclbar. CH.sub.2 --COOR.sub.2yto obtain a compound of the formula ##STR5## in (S) enantiomeric form, wherein R.sub.2x is primary or secondary C.sub.1-4 alkyl, benzyl or allyl,R.sub.2y is C.sub.1-4 alkyl not containing an asymmetric carbon atom, andR.sub.3 ' is methyl or ethyl,processes for the synthesis of compounds of the formula ##STR6## comprising reacting a compound of the formula ##STR7## with the reaction product of a strong base and a compound of the formula ##STR8## optionally followed by, when R.sub.2z is allyl, cleavage of the allyl and P.sub.1 groups to obtain the corresponding compound of the formula ##STR9## wherein each R.sub.7 is methyl or ethyl,R is as defined in the specification, and eachP.sub.1 independently and R.sub.2z are as defined above, andthe compounds of the formula ##STR10## wherein R and each R.sub.7 are as defined above.
摘要翻译：用于合成R [R *，S *]对映体形式的式“IMAGE”的化合物的方法，其中每个P1独立地是羟基保护基，R2z是C1-4烷基，苄基或烯丙基，包括作为 R2z为R2x时的关键步骤，式（S）对映异构形式的式（IMA）化合物与式Mg＆cir＆+2（（ - ）OOC-CH2-COOR2x）2的化合物的反应，得到化合物式（S）对映体形式的式（IMAGE）式中，作为R2z为R2y的关键步骤，式（S）对映异构体形式的式“IMAGE”的化合物与式Li ）（ - ）CH2-COOR2y，得到（S）对映异构体形式的下式的化合物，其中R2x是伯或仲C 1-4烷基，苄基或烯丙基，R2y是不含不对称碳原子的C 1-4烷基，并且R 3'是甲基或乙基，用于合成式IMA化合物的方法包括使式IMA的化合物与强碱的反应产物 da化合物，其中当R 2z是烯丙基时，烯丙基和P1基团裂解，得到相应的式“IMAGE”化合物，其中每个R 7是甲基或乙基，R如说明书中所定义，每个P1独立地和R2z如上所定义，并且式“IMAGE”的化合物其中R和每个R 7如上所定义。

7. 发明授权

US4338079A Method and apparatus for subjecting mineral particles to gas flow 失效
标题翻译：使矿物颗粒气体流动的方法和装置
公开(公告)号：US4338079A
公开(公告)日：1982-07-06
申请号：US219998
申请日：1980-12-23
申请人： Bobby P. Faulkner , George T. Lee , Peter L. Schumacher , Michael H. Weinecke
发明人： Bobby P. Faulkner , George T. Lee , Peter L. Schumacher , Michael H. Weinecke
IPC分类号： B01J8/10 , F26B3/00 , F26B3/06 , F26B17/00 , F26B17/28 , F27B9/24 , F27B15/00 , F27B15/02
CPC分类号： F26B3/06 , B01J8/10 , F26B17/28 , F27B15/00 , F27B15/02 , F27B9/2407 , B01J2219/182
摘要： Roller grate method and apparatus for simultaneously transporting, agitating and exchanging heat with a bed of solid mineral particles has elongated cylindrical horizontal rollers with gas passage apertures therethrough, a hopper for feeding mineral particles onto the rollers and forming a bed having a depth several times greater than the average diameter of the particles; a drive source to rotate the rollers and frictionally engage the cylindrical surfaces with the particles in the lowermost layer of the bed and urge the bed along a path of travel transverse to the axes of the rollers; elongated filler members disposed in the nip between adjacent rollers to prevent the particles from jamming the rollers and to provide resistance to the flow of the bed along said path of travel; and a heat chamber spanning the rollers and a fan for forcing a heat transfer gas stream through the gas passage apertures in the rollers and through the bed as it is being transported, the rollers and the filler members being adapted to continually agitate the particles and to slowly transport the bed past the gas stream at a velocity which is only a minor fraction of the peripheral velocity of the rollers.
摘要翻译：用于与固体矿物颗粒床同时运输，搅拌和交换热量的辊式炉排方法和装置具有细长的圆柱形水平辊，其中具有气体通道孔，用于将矿物颗粒馈送到辊上并形成深度几倍的床的料斗比颗粒的平均直径; 驱动源，用于旋转辊子并且将圆柱形表面与床的最下层中的颗粒摩擦接合，并沿着横向于辊的轴线的行进路径推动床; 细长的填料构件设置在相邻辊之间的辊隙中，以防止颗粒堵塞辊并且沿着所述行进路径提供对床的流动的阻力; 以及跨过辊的加热室和用于迫使传热气流通过辊中的气体通道孔并在其被输送时通过床的风扇，辊和填料构件适于连续地搅拌颗粒，并且缓慢地以超过滚筒圆周速度的一小部分的速度将床流过气流。

8. 发明授权

US4270899A Roller grate material bed transporting and heat exchange apparatus 失效
标题翻译：辊式炉料运输和热交换装置
公开(公告)号：US4270899A
公开(公告)日：1981-06-02
申请号：US105982
申请日：1979-12-21
申请人： Bobby P. Faulkner , George T. Lee , Peter L. Schumacher , Michael H. Weinecke
发明人： Bobby P. Faulkner , George T. Lee , Peter L. Schumacher , Michael H. Weinecke
IPC分类号： F27B9/24 , F27B15/00 , F26B19/00
CPC分类号： F27B9/2407 , B01J2219/182 , Y10S198/95
摘要： Roller grate apparatus for simultaneously transporting and transferring heat to or from a bed of material particles has elongated cylindrical parallel horizontal rollers rotatably driven in the same direction; filler bars disposed in the nip between adjacent rollers and together with the rollers forming a generally flat surface with constantly moving portions which continually tumble the material particles and urge them thereacross in a direction transverse to the roller axes; gas passage apertures in the rollers which permit a heat transfer gas stream to pass through the rollers; a heat transfer chamber spanning the rollers; and a fan for blowing a heat transfer gas stream through the chamber and the material bed being transported by the rollers.
摘要翻译：用于同时传送和传送热量到材料颗粒床的辊式炉排装置具有沿相同方向可旋转地驱动的细长圆柱形平行水平辊; 填充棒设置在相邻辊之间的辊隙中并且与滚子一起形成大致平坦的表面，其具有不断移动的部分，其连续地滚动材料颗粒并且在横向于辊轴线的方向上将它们推向它们; 辊中的气体通道孔允许传热气体流通过辊子; 跨越辊的传热室; 以及用于吹送传热气体流通过所述室和由所述辊传送的所述材料床的风扇。

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