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1.发明授权Crystals of N-(trans-4-isopropylcyclohexycarbonyl)-D-phenylalanine and methods for preparing them 失效N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的晶体及其制备方法
公开(公告)号：US5488150A
公开(公告)日：1996-01-30
申请号：US166144
申请日：1993-12-14
IPC分类号： C07C231/24 , A61K31/13 , A61K31/195 , C07C211/43 , C07C231/22 , C07C233/63 , C07C239/00
CPC分类号： C07C231/22 , C07C233/63
摘要： Stable crystals of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine may be produced by treating this compound with a solvent at a temperature of at least 10.degree. C. and forming crystals in the solvent at a temperature of at least 10.degree. C. For example, crystals may be formed by crystallization out of solution, or may be formed from solid particles of the compound suspended in a solvent. Crystals formed in this way have different melting point, infra red spectrum and X-ray diffraction patterns from previously known forms of the compound and have enhanced processability, eg. stability to grinding.
摘要翻译： N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的稳定晶体可以通过在至少10℃的温度下用溶剂处理该化合物并在溶剂中在至少10℃的温度下形成晶体来制备 例如，可以通过从溶液中结晶而形成晶体，或者可以由悬浮在溶剂中的化合物的固体颗粒形成晶体。 以这种方式形成的晶体具有来自先前已知形式的化合物的不同的熔点，红外光谱和X射线衍射图，并具有增强的可加工性，例如。 稳定磨削。
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2.发明授权Crystals of N- (trans-4-isopropylcyclohexlycarbonyl)-D-phenylalanine and methods for preparing them 失效N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的晶体及其制备方法
公开(公告)号：US5463116A
公开(公告)日：1995-10-31
申请号：US190460
申请日：1994-02-02
IPC分类号： C07C231/22 , C07C233/63 , C07C229/00
CPC分类号： C07C231/22 , C07C233/63 , C07B2200/13 , C07C2101/14
摘要： Stable crystals of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine may be produced by treating this compound with a solvent at a temperature of at least 10.degree. C. and forming crystals in the solvent at a temperature of at least 10.degree. C. For example, crystals may be formed by crystallization out of solution, or may be formed from solid particles of the compound suspended in a solvent. Crystals formed in this way have different melting point, infra red spectrum and X-ray diffraction patterns from previously known forms of the compound and have enhanced processability, e.g., stability to grinding.
摘要翻译： N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的稳定晶体可以通过在至少10℃的温度下用溶剂处理该化合物并在溶剂中在至少10℃的温度下形成晶体来制备 例如，可以通过从溶液中结晶而形成晶体，或者可以由悬浮在溶剂中的化合物的固体颗粒形成晶体。 以这种方式形成的晶体具有来自先前已知形式的化合物的不同的熔点，红外光谱和X射线衍射图，并且具有增强的加工性，例如研磨的稳定性。
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公开(公告)号：US4942255A
公开(公告)日：1990-07-17
申请号：US301445
申请日：1989-01-25
申请人： Satoji Takahashi , Tadashi Takemoto
发明人： Satoji Takahashi , Tadashi Takemoto
IPC分类号： A23L27/30 , B01J23/06 , B01J27/053 , B01J27/122 , B01J27/232 , B01J31/02 , B01J31/04 , B01J31/08 , C07B61/00 , C07K1/02 , C07K5/075 , C07K5/117
CPC分类号： C07K5/0613
摘要： A method for producing an .alpha.-aspartylphenylalanine derivative represented by formula (2), which comprises reacting a .beta.-aspartylphenylalanine derivative represented by formula (1): ##STR1## with a basic compound in an alcohol solvent in the presence of a hydroxide, sulfate, chloride, carbonate or acetate of an element selected from the group consisting of zinc, copper, nickel, magnesium, aluminum, iron, tin, silicon and titanium, wherein R.sub.1 and R.sub.2 represent hydrogen or an alkyl group having 1 to 4 carbon atoms.
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公开(公告)号：US4904802A
公开(公告)日：1990-02-27
申请号：US202565
申请日：1988-06-06
申请人： Satoji Takahashi , Tadashi Takemoto
发明人： Satoji Takahashi , Tadashi Takemoto
IPC分类号： C07D207/416 , C07K1/02 , C07K5/075 , C07K5/078
CPC分类号： C07K5/06139 , Y02P20/582
摘要： An imide of the formula: ##STR1## where R.sub.1 is hydrogen or C.sub.1-4 alkyl.
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5.发明授权Method for production of N-protected-alpha-L-aspartyl-L-phenylalanine methyl ester 失效N-保护-α-L-天冬氨酰基-L-苯丙氨酸甲酯的制备方法
公开(公告)号：US4824994A
公开(公告)日：1989-04-25
申请号：US650498
申请日：1984-09-14
申请人： Satoji Takahashi , Katsumi Sugiyama
发明人： Satoji Takahashi , Katsumi Sugiyama
IPC分类号： C07K1/02 , C07K5/075 , C07C101/02
CPC分类号： C07K5/0613
摘要： A method for the production of N-carbobenzoxy-.alpha.-L-aspartyl-L-phenylalanine methyl ester characterized by the reaction of L-phenylalanine methyl ester with fine N-carbobenzoxy-L-aspartic anhydride crystals, is disclosed.
摘要翻译： 公开了生产N-苄氧羰基-α-天冬氨酰基-L-苯丙氨酸甲酯的方法，其特征在于L-苯丙氨酸甲酯与N-苄氧羰基-L-天冬氨酸精氨酸晶体的精细反应。
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公开(公告)号：US08362244B2
公开(公告)日：2013-01-29
申请号：US11782695
申请日：2007-07-25
IPC分类号： C07D473/34 , C07D473/30
CPC分类号： C12P17/182 , C07D473/30 , C07D473/34 , Y02P20/55
摘要： The present invention relates to a method for producing a nucleoside derivative represented by formula (2), comprising the step of reducing a nucleoside of formula (1) in the presence of a noble metal catalyst comprising a carrier and a noble metal supported thereby, selected from the group consisting of (A) a homogeneously supported catalyst where the specific surface area of the noble metal is 95.0 m2/g or more and the particle size of the noble metal is 4.3 nm or less, and (B) a surface-loaded catalyst where the specific surface area of the noble metal is 56.0 m2/g or more and the particle size of the noble metal is 8.0 nm or less, wherein R1 is hydrogen or a protective group, R2 is NH2 or OH, R3 is an acyl group, and X is a chlorine or bromine atom. According to the present invention, the yield can be made equal even when the amount of catalyst is smaller than that used for the conventional products.
摘要翻译： 本发明涉及一种制备由式（2）表示的核苷衍生物的方法，包括在贵金属催化剂存在下还原式（1）的核苷的步骤，所述贵金属催化剂包含载体和由其所支持的贵金属，所选择的贵金属被选择 由（A）贵金属的比表面积为95.0m 2 / g以上，贵金属的粒径为4.3nm以下的均匀负载的催化剂组成的组，（B）表面负载型 贵金属的比表面积为56.0m 2 / g以上，贵金属的粒径为8.0nm以下的催化剂，其中，R1为氢或保护基，R2为NH2或OH，R3为酰基 基团，X是氯或溴原子。 根据本发明，即使当催化剂的用量小于常规产品所用量时，产率也可以相等。
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公开(公告)号：US20070167523A1
公开(公告)日：2007-07-19
申请号：US11686073
申请日：2007-03-14
IPC分类号： A61K31/198 , C07C237/20
CPC分类号： C07C231/02 , C07C231/24 , C07C2601/14 , C07C233/63
摘要： There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.
摘要翻译： 提供了那格列奈晶体的制备方法，其包括以下步骤：向含有那格列奈的反应混合物中加入酸以使其呈酸性，反应混合物通过反式-4-异丙基环己基羰基氯与D-苯丙氨酸反应获得 酮溶剂和水的混合溶剂在碱的存在下; 然后将混合物的温度调节至58℃至72℃，酮溶剂的浓度大于8重量％且小于22重量％，以进行那格列奈晶体的沉淀。 这种生产方法是奈格列奈结晶的工业上有益的方法。
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公开(公告)号：US5362903A
公开(公告)日：1994-11-08
申请号：US152134
申请日：1993-11-16
申请人： Shinji Fujita , Satoji Takahashi
发明人： Shinji Fujita , Satoji Takahashi
IPC分类号： C07K1/14 , C07K5/072 , C07K5/075 , C07C103/52
CPC分类号： C07K5/0613
摘要： This invention is directed to provide a method for obtaining .alpha.-L-aspartyl-L-phenylalanine selectively in high yields. Diffusion dialysis with an ion exchange membrane is used to decrease hydrochloric acid concentration of a mixed solution containing hydrochloric acid and one or more of four .alpha.-L-aspartyl-L-phenylalanine derivatives, i.e., .alpha.-L-aspartyl-L-phenylalanine methyl ester, .alpha.-L-aspartyl-L-phenylalanine, .alpha.-L-aspartyl-L-phenylalanine-.beta.-methyl ester and .alpha.-L-aspartyl-L-phenylalanine dimethyl ester. The resultant solution is concentrated, to which a base is added for neutralization. Subsequently, .alpha.-L-aspartyl-L-phenylalanine is crystallized and isolated.
摘要翻译： 本发明旨在提供以高产率选择性地获得α-L-天冬氨酰基-L-苯丙氨酸的方法。 使用离子交换膜的扩散透析用于降低含有盐酸和四种α-L-天冬氨酰基-L-苯丙氨酸衍生物中的一种或多种的混合溶液的盐酸浓度，即α-L-天冬氨酰基-L-苯丙氨酸甲酯 酯，α-L-天冬氨酰基-L-苯丙氨酸，α-L-天冬氨酰基-L-苯丙氨酸-β-甲酯和α-L-天冬氨酰基-L-苯丙氨酸二甲酯。 将所得溶液浓缩，向其中加入碱进行中和。 随后，将α-L-天冬氨酰基-L-苯丙氨酸结晶并分离。
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公开(公告)号：US07208622B2
公开(公告)日：2007-04-24
申请号：US10418105
申请日：2003-04-18
IPC分类号： C07C229/00
CPC分类号： C07C231/02 , C07C231/24 , C07C2601/14 , C07C233/63
摘要： There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.
摘要翻译： 提供了那格列奈晶体的制备方法，其包括以下步骤：向含有那格列奈的反应混合物中加入酸以使其呈酸性，反应混合物通过反式-4-异丙基环己基羰基氯与D-苯丙氨酸反应获得 酮溶剂和水的混合溶剂在碱的存在下; 然后将混合物的温度调节至58℃至72℃，酮溶剂的浓度大于8重量％且小于22重量％，以进行那格列奈晶体的沉淀。 这种生产方法是奈格列奈结晶的工业上有益的方法。
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公开(公告)号：US5451671A
公开(公告)日：1995-09-19
申请号：US76964
申请日：1993-06-16
申请人： Hiroshi Shiragami , Masayuki Arai , Kunisuke Izawa , Yutaka Honda , Yasuhiro Tanaka , Toshihide Yukawa , Satoji Takahashi
发明人： Hiroshi Shiragami , Masayuki Arai , Kunisuke Izawa , Yutaka Honda , Yasuhiro Tanaka , Toshihide Yukawa , Satoji Takahashi
IPC分类号： C07H1/06 , C07H19/04 , C07H19/173
摘要： A crude 2',3'-dideoxynucleoside compound is purified by extracting with an organic solvent, or crystallizing, the 2',3'-dideoxynucleoside compound from a basic aqueous solution having a pH of not less than 12 containing the same. In another embodiment of purification a basic aqueous solution having a pH of not less than 11 of a crude 2',3'-dideoxynucleoside derivative is brought into contact with a nonpolar porous resin, whereby the derivative is adsorbed on the resin, and then the thus adsorbed derivative is desorbed with an aqueous alcoholic solution.2',3'-Dideoxynucleoside compounds which have utility as anti-AIDS drugs or anti-virus drugs can be isolated and purified in high purity and in high yield from their crude products containing impurities.
摘要翻译： 粗制的2'，3'-二脱氧核苷化合物通过用有机溶剂萃取，或从含有其的pH不低于12的碱性水溶液中结晶2'，3'-二脱氧核苷化合物而纯化。 在纯化的另一个实施方案中，使粗制的2'，3'-二脱氧核苷衍生物的pH不低于11的碱性水溶液与非极性多孔树脂接触，由此将衍生物吸附在树脂上，然后将 因此吸附的衍生物用含水醇溶液解吸。 具有作为抗艾滋病药物或抗病毒药物的作用的2'，3'-二脱氧核苷化合物可以从其含有杂质的粗产物中以高纯度和高产率分离和纯化。
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