levonorgestrel | 797-63-7

• 物质功能分类: 原料药 - 激素及调节内分泌功能类药 - 避孕药
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: levonorgestrel
• 英文别名: D(-)norgestrel；D-norgestrel；norgestrel；17β-Hydroxy-3-oxo-13β-ethyl-17α-ethinyl-gonen-(4)；(8R,9R,10R,13S,14R,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one；(8R,9S,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
• CAS: 797-63-7；797-64-8；6533-00-2；17092-09-0
• 化学式: C₂₁H₂₈O₂
• 分子量: 312.452
• InChiKey: WWYNJERNGUHSAO-XZCODKSBSA-N

物化性质

• 熔点：
  239-241 °C(lit.)
• 沸点：
  392.36°C (rough estimate)
• 密度：
  1.0697 (rough estimate)
• 溶解度：
  氯仿（少量，超声处理）、二氯甲烷（少量溶解）、甲醇（少量溶解）
• 颜色/状态：
  Crystals from methanol
• 蒸汽压力：
  1.0X10-9 mm Hg at 25 °C (est)
• 分解：
  When heated to decomposition, it emits acrid smoke and irritating fumes.
• 稳定性/保质期：

  在常温常压下稳定。

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

ADMET

代谢

(14)C-Norgestrel 给七名受试者服用后，5天内尿液中排出了43%的剂量... 酶水解只释放了尿液中32%的放射性，另外25%以硫酸盐结合物的形式排出。尿液中排出的代谢物比服用相关化合物如norethisterone或lynestrenol后的代谢物极性要小得多。从尿液中分离并鉴定出了四氢诺孕醇的3alphaOH,5beta和3betaOH,5beta异构体（13beta-乙基-17alpha-乙炔基-5beta-孕烷-3alpha,17beta-二醇），通过质谱、薄层色谱和气液色谱进行了鉴定。血浆中放射性活性下降速度比服用norethisterone和lynestrenol后更快。大约2%的服用剂量转化为了酸性化合物。无论是口服还是静脉注射norgestrel，放射性排出速率或代谢物没有明显差异。

(14)C-Norgestrel was administered to seven human subjects and 43% of dose was excreted in the urine within 5 days ... Enzymic hydrolysis released only 32% of the urinary radioactivity and a further 25% was excreted as sulphate conjugates. The metabolites excreted in the urine were much less polar than those following the administration of the related compounds, norethisterone or lynestrenol. The 3alphaOH,5beta and 3betaOH,5beta isomers of the tetrahydronorgestrel (13beta-ethyl-17alpha-ethynyl-5 beta-gonane-3alpha,17beta-diol) were isolated from urine and identified by mass spectrometry and thin-layer and gas-liquid chromatography. Plasma radioactivity decreased more rapidly than after the administration of norethisterone and lynestrenol. About 2% of the administered dose was converted to acidic compounds. There was no apparent difference in the rate of excretion of radioactivity or in the metabolites after either oral or intravenous administration of norgestrel.

来源:Hazardous Substances Data Bank (HSDB)

代谢

在本研究中，我们调查了非洲绿猴（Cercopithecus aethiops）对dl-、d-和l-诺孕醇的代谢比较。单次口服给予(14)C-dl-诺孕醇（1 mg/kg）后，尿液中的总(14)C排泄量显著高于给予d-对映体后的排泄量（51.4 +/- 5.0% 对 37.5 +/- 5.4%），但与给予l-对映体后的排泄量（44.2 +/- 8.9%）无显著差异。在所有情况下，尿液中放射性物质的主要部分以游离分数存在（48-62%），此外，通过β-葡萄糖醛酸酶制剂释放的放射性物质占13-27%。未检测到硫酸盐结合物。至少有一个主要（16beta-羟基化）和一个次要（16alpha-羟基化）的代谢途径是立体选择性的，即它们在l-对映体而非d-对映体上起作用。三种代谢物，16beta-羟基诺孕醇、16alpha-羟基诺孕醇和16-羟基四氢诺孕醇（被认为是16beta）仅在给予(14)C-dl-和-l-诺孕醇的动物尿样中检测到。在给予(14)C-d-诺孕醇后，3alpha, 5beta-四氢诺孕醇被确定为主要的尿液代谢物。这些观察结果与之前在女性尿液中dl-诺孕醇代谢物的报告进行了比较。

The comparative metabolism of dl-, d-, and l-norgestrel was investigated in African Green Monkeys (Cercopithecus aethiops). Total (14)C excretion in urine after a single oral dose of (14)C-dl-norgestrel (1 mg/kg) was significantly higher (51.4 +/- 5.0%) than that observed after administration of the d-enantiomer (37.5 +/- 5.4%) but not the l-enantiomer (44.2 +/- 8.9%). In all cases, the major part of the urinary radioactivity was present in a free fraction (48-62%), while an additional 13-27% was released by beta-glucuronidase preparations. No sulfate conjugates were detected. At least one major (16beta-hydroxylation) and one minor (16alpha-hydroxylation) metabolic pathway were stereoselective, i.e., they are operative with the I-but not the d-enantiomer. Three metabolites, 16beta-hydroxynorgestrel, 16alpha-hydroxynorgestrel, and 16-hydroxytetrahydronorgestrel (believed to be 16beta) were only detected in urine samples obtained from (14)C-dland -l-norgestrel-dosed animals. Following (14)C-d-norgestrel administration, 3alpha, 5beta-tetrahydronorgestrel was found to be the major urinary metabolite. These observations are compared with those reported earlier on the urinary metabolites of dl-norgestrel in women.

来源:Hazardous Substances Data Bank (HSDB)

代谢

体外对诺孕醇立体异构体（D型、L型以及外消旋混合物DL）的代谢进行了研究，使用的是兔肝微粒体部分。生物活性较强的L-诺孕醇的代谢速度比生物活性较低的D-诺孕醇快，这主要是由于L-诺孕醇更容易转化为环A还原代谢物。两种异构体在羟基化方面的量没有差异；大约30%的每种异构体在30分钟孵化后被转化为羟基化代谢物。然而，两种异构体在转化方面存在差异，L-诺孕醇主要转化为16beta-羟基甾体，而D-诺孕醇转化为16alpha-羟基甾体。两种异构体在C-6位置上的羟基化量相似。外消旋混合物的代谢速度介于D型和L型异构体之间。

The in vitro metabolism of stereo-isomers (d, l and the racemic mixture dl) of norgestrel by a microsomal fraction from rabbit liver was investigated. The metabolism of the biologically active l-norgestrel was more rapid than that of d-norgestrel (sic.) which is biologically inactive. This was mainly due to the more ready conversion of l-norgestrel to ring-A reduced metabolites. There was no difference between the two isomers in respect of the amount undergoing hydroxylation; about 40% of each isomer was converted to hydroxylated metabolites after 30 min incubation. However, there were differences between the isomers, l-norgestrel being converted mainly to the 16beta-hydroxysteroid and d-norgestrel to the 16alpha-hydroxysteroid. Similar amounts of both isomers were hydroxylated at C-6. The metabolism of the racemic mixture was intermediate between that of the d and l isomers.

来源:Hazardous Substances Data Bank (HSDB)

代谢

19-去甲睾酮衍生的合成孕激素在大白兔体外肝脏组织中的代谢速率进行了比较。在1小时的时间范围内，炔诺酮的代谢速度与19-去甲睾酮相当，而d-诺孕酯和利奈孕醇的代谢速度略低。不到5%的l-诺孕酯被代谢。在所有情况下，反应产物都是四氢孕激素。利奈孕醇通过炔诺酮代谢。骨骼肌、肺和小肠也能代谢炔诺酮和d-诺孕酯，但速率比肝脏组织慢。少量炔诺酮被脂肪组织代谢，但心脏和脾脏无活性。利奈孕醇和l-诺孕酯没有被研究的任何一种肝外组织代谢。

The rates of metabolism of synthetic gestagens derived from 19-nortestosterone by rabbit liver tissue in vitro were compared. Over a period of 1 hr norethisterone was metabolized as rapidly as 19-nortestosterone whereas d-norgestrel and lynestrenol were metabolized at a slightly lower rate. Less than 5% of l-norgestrel was metabolized. In all cases the reaction product was the tetrahydrosteroid. Lynestrenol was metabolised through norethisterone. Skeletal muscle, lung and small intestine also metabolized norethisterone and d-norgestrel but at a slower rate than liver tissue. Small amounts of norethisterone were metabolized by adipose tissue but heart and spleen were inactive. Lynestrenol and l-norgestrel were not metabolized by any of the extra-hepatic tissues studied.

来源:Hazardous Substances Data Bank (HSDB)

代谢

体外研究对三种在口服避孕药（OCs）中使用的类固醇激素进行了研究，通过小块的人类空肠粘膜来观察其代谢情况。这样做是因为人类的胃肠粘膜已知能够代谢多种药物。经过培养后，几乎有40%的炔雌醇、9.8%的左炔诺孕酮和7%的甲基炔诺酮被代谢。所有这些代谢反应与对照组有显著差异。研究结果表明，炔雌醇的代谢与所用组织的重量有关。这些结果与炔雌醇已知的显著首次通过效应一致。已知诺孕酯具有很小或没有首次通过效应，因此没有显示出高的肠道代谢率。在所使用的实验条件下，炔雌醇或左炔诺孕酮的I相代谢并不明显。

In vitro studies were conducted on the metabolism of 3 steroids used in OCs (oral contraceptives) by small pieces of human jejunal mucosa. This was done because the gastrointestinal mucosa of humans is known to metabolize a number of drugs. Almost 40% of the ethinyl estradiol, 9.8% of the levonorgestrel, and 7% of the mestranol were metabolized after incubation. All these metabolic responses were significantly different from those in the control groups. Results of the study show that the metabolism of the ethinyl estradiol was related to the weight of the tissue used. These results are consistent with the known marked 1st pass effect of ethinyl estradiol. Norgestrel, known to have little or no 1st pass effect, did not show a high rate of gut metabolism. Under the experimental conditions employed, no Phase 1 metabolism of either ethinyl estradiol or levonorgestrel was apparent.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

炔雌醇和孕激素的代谢可能会被同时使用的已知诱导药物代谢酶的物质增加，特别是细胞色素P450酶，例如抗惊厥药（例如苯巴比妥、苯妥英、卡马西平）和抗感染药（例如利福平、利福布汀、奈韦拉平、依非韦伦）。

The metabolism of estrogens and progestagens may be increased by concomitant use of substances known to induce drug-metabolising enzymes, specifically cytochrome P450 enzymes, such as anticonvulsants (eg phenobarbital, phenytoin, carbamazepine), and anti-infectives (eg rifampicin, rifabutin, nevirapine, efavirenz).

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

利托那韦和奈非那韦虽然被认为是强烈的抑制剂，但与之相反，当与类固醇激素同时使用时，它们表现出诱导性质。

Ritonavir and nelfinavir, although known as strong inhibitors, by contrast exhibit inducing properties when used concomitantly with steroid hormones.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

含有圣约翰草（金丝桃）的草药制剂可能会诱导雌激素和黄体激素的代谢。

Herbal preparations containing St John's Wort (Hypericum Perforatum) may induce the metabolism of estrogens and progestagens.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

苯妥英和利福平增加性激素结合球蛋白（SHBG）的血清浓度；这显著降低了一些孕激素的自由药物血清浓度，这对于使用孕激素进行避孕的患者来说是一个特别关注的问题。/孕激素/

Phenytoin and rifampin increase the serum concentrations of sex hormone-binding globulin (SHBG); this significantly decreases the serum concentration of free drug for some progestins, which is a special concern in patients using progestins for contraception. /Progestins/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

药物相互作用数据对于利福布汀尚不可用，但由于其结构与利福平相似，因此在与孕激素联合使用时可能需要类似的谨慎措施。

Drug interaction data are not available for rifabutin, but because its structure is similar to that of rifampin, similar precautions with its use with progestins may be warranted. ... /Progestins/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

左炔诺孕酮通过胃肠道吸收，在肝脏代谢，并以葡萄糖醛酸和硫酸盐结合物的形式通过尿液和粪便排出。

Norgestrel is absorbed from the gastrointestinal tract, metabolised by the liver and excreted in the urine and faeces as glucuronide and sulphate conjugates.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

(14)C-Norgestrel 给七名受试者服用后，5天内尿液中排出了剂量的43%；放射性物质的生物学半衰期是24小时。酶水解仅释放了尿液中放射活性的32%，另外25%以硫酸结合物形式排出。尿液中排出的代谢物相比服用相关化合物如炔雌醇或利奈孕酮后排出的代谢物极性要小得多。从尿液中分离出了四氢诺孕醇的3alphaOH,5beta和3betaOH,5beta异构体（13beta-乙基-17alpha-乙炔基-5beta-孕烷-3alpha,17beta-二醇），并通过质谱、薄层色谱和气液色谱进行了鉴定。血浆中放射活性的下降速度比服用炔雌醇和利奈孕酮后要快。大约2%的服用剂量转化为了酸性化合物。无论是口服还是静脉给药，诺孕醇放射性物质排出速率或代谢物没有明显差异。

(14)C-Norgestrel was administered to seven human subjects and 43% of dose was excreted in the urine within 5 days; the biological half-life of the radioactivity was 24 hr. Enzymic hydrolysis released only 32% of the urinary radioactivity and a further 25% was excreted as sulphate conjugates. The metabolites excreted in the urine were much less polar than those following the administration of the related compounds, norethisterone or lynestrenol. The 3alphaOH,5beta and 3betaOH,5beta isomers of the tetrahydronorgestrel (13beta-ethyl-17alpha-ethynyl-5 beta-gonane-3alpha,17beta-diol) were isolated from urine and identified by mass spectrometry and thin-layer and gas-liquid chromatography. Plasma radioactivity decreased more rapidly than after the administration of norethisterone and lynestrenol. About 2% of the administered dose was converted to acidic compounds. There was no apparent difference in the rate of excretion of radioactivity or in the metabolites after either oral or intravenous administration of norgestrel.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

不同合成类固醇（用于激素避孕）与性激素结合球蛋白（SHBG）的结合能力通过测量它们在竞争性蛋白结合系统中取代放射性标记的睾酮的能力进行研究。只有19-去甲睾酮衍生物具有显著取代睾酮的能力，d-诺孕酯（d-Ng）是最强的取代剂。在SHBG水平增加的女性中，之前恒定的血浆d-Ng水平增加了两到六倍。因此，可以得出结论，SHBG是d-Ng的主要载体蛋白。d-Ng强烈的睾酮取代活性也可能解释含d-Ng的口服避孕药观察到的雄激素样副作用。

The binding of different synthetic steroids, used in hormonal contraception, to Sex Hormone Binding Globulin (SHBG) was studied by measuring their ability to displace tritiated testosterone from SHBG in a competitive protein binding system. Only 19-nortestosterone derivates had any significant ability to displace testosterone from SHBG, d-norgestrel (d-Ng) being the strongest displacer. Increasing the SHBG levels in women with previous constant plasma d-Ng levels increased these levels two- to sixfold. It is concluded that SHBG is the main carrier protein for d-Ng. The strong testosterone displacing activity of d-Ng might also explain androgenic side effects observed with d-Ng containig oral contraceptives.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S22,S36
• 危险类别码：
  R20/21/22,R40
• WGK Germany：
  3
• 海关编码：
  2937290090
• 储存条件：
  常温、避光、存放在通风干燥处。

制备方法与用途

概述

左炔诺孕酮是一种速效、短期口服避孕药，通过显著抑制排卵和阻止孕卵着床，并使宫颈黏液稠度增加，精子穿透阻力增大，从而发挥速效避孕作用。目前，单用孕激素或与雌激素配伍的左炔诺孕酮已制成多种类型的女性避孕药，以口服、外用及注射等方式达到避孕目的。

药理作用

左炔诺孕酮是一种强效孕激素，其孕激素作用约为炔诺酮的5～10倍，并具有雄激素和抗雌激素活性。该药物主要通过抑制排卵来发挥作用。此外，它还能改变宫颈黏液性质，使精子难以穿透；同时，它还可以使子宫内膜变薄，不利于受精卵着床。

用法用量

• 短效口服避孕药：从月经第5天开始，每天服1片（丸），连服22天。停药后2～4天来月经，然后于第5天继续服用下一个月的药。
• 探亲避孕药：于探亲当晚开始服炔诺孕酮探亲避孕药，每天1片，服法同短效口服避孕药。
• 事后避孕药：房事后72小时内口服2片复方炔诺孕酮事后避孕片，12小时后再服2片。

不良反应

常见不良反应包括胃纳差、痤疮、液体潴留和水肿、体重增加、过敏性皮肤炎症、精神压抑、乳房疼痛、女性性欲改变、月经紊乱、不规则出血或闭经。少见的不良反应有头痛，胸、臀、腿特别是腓肠肌处疼痛，手臂和脚无力、麻木或疼痛，突然的或原因不明的呼吸短促，突然语言发音不清，突然视力改变、复视、不同程度失明等。长期应用可能引起肝功能异常，缺血性心脏病发生率上升，妊娠早期时应用可能导致雄激素活性高引起的后代女婴男性化以及生殖道畸形（多见为尿道下裂）。

药物相互作用

• 与利福平、氯霉素、氨苄西林、苯巴比妥、苯妥英钠、扑米酮、甲丙氨酯、氯氮平、对乙酰氨基酚及吡唑酮类镇痛药（保泰松）等同服可产生肝微粒体酶效应，加速炔酮在体内的代谢，导致避孕失败、突破性出血发生率增高。
• 维生素C能增强口服避孕药的作用，每天口服1g维生素C可使炔雌醇生物利用度从40%提高到60%～70%。
• 与环孢素合用，可抑制环孢素的代谢清除，致其毒性增强，应避免合用。

规格

• 复方炔诺孕酮一号片（或滴丸）：每片（丸）含炔诺孕酮0.3mg和炔雌醇0.03mg。
• 炔诺孕酮探亲避孕片：每片含炔诺孕酮3mg。
• 复方炔诺孕酮事后避孕片：每片含炔诺孕酮1mg和炔雌醇0.1mg。

化学性质

左炔诺孕酮为白色或类白色结晶性粉末，无臭、无味。不溶于水，溶于氯仿，微溶于甲醇。

用途

用于避孕药。

反应信息

• 作为反应物：
  描述：

  levonorgestrel 在 silver carbonate 作用下， 以 甲苯 为溶剂， 反应 1.5h， 以100%的产率得到D-(+)-13β-ethylgon-4-ene-3,17-dione
  参考文献：
  名称：

  (17α,20E/Z)-iodovinyl- and 16α-iodo-18-homoestradiol derivatives: synthesis and evaluation for estrogen receptor imaging

  摘要：

  Three new I-125-radioiodinated estrogens featuring a 13 beta-ethyl instead of the natural 13-methyl group, i.e. 18-homoestradiols, were synthesized and evaluated as potential estrogen receptor imaging agents. The 16 alpha-iodo-18-methylestradiol and the I-125-labeled analog were synthesized from the corresponding 16 beta-bromo analog by the halogen-exchange method. The cis-bromohydrin precursor was obtained by bromination of an estrone enolacetate, followed by epimerization and reduction. The isomeric (17 alpha,20E/Z)-iodovinyl-18-methylestradiols were prepared via the vinyltin intermediates. Treatment of 18-methyl-17 alpha-ethynylestradiol with tri-n-butyltin hydride, in the presence of azobisisobutyronitrile as catalyst and heating at 90-100 degrees C afforded the (17 alpha,20E)-tri-n-butylstannyl isomer as the major product. Changing the catalyst for triethyl borane, at room temperature, mainly gave the 20Z-isomer. The nea I-125-labeled analogs were obtained from their corresponding tin intermediates upon treatment with [I-125]NaI in the presence of H2O2. The 16 alpha-[I-125]iodo- and isomeric (17 alpha,20E/Z)-[I-125]iodovinyl-18-methylestradiols were evaluated for estrogen receptor-mediated uterine uptake in immature female rats. Homologation of the C13-methyl group did improve the uterine uptake of the iodovinyl derivatives, but also increased blood retention, resulting in lower target uptake ratios. In the case of the 16 alpha-iodo analog uterine retention decreased upon C13-homologation. (C) 2000 Elsevier Science Inc. All rights reserved.

  DOI：

  10.1016/s0039-128x(99)00084-7
• 作为产物：
  描述：

  沃氏物 、 三甲基乙炔基硅 在 正丁基锂 、 水 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 4.0h， 以93.6%的产率得到levonorgestrel
  参考文献：
  名称：

  左炔诺孕酮的合成方法

  摘要：

  本发明涉及一种左炔诺孕酮的合成方法，以式(Ⅰ)化合物为原料，采用一锅法合成左炔诺孕酮，减少了中间体分离纯化操作，生产过程大大简化，且反应速度快，生产周期短；且该合成方法无需使用乙炔气体，安全性较好，收率较高，生产成本较低，适合大规模工业生产。

  公开号：

  CN114181272A

文献信息

• Process for the synthesis of high purity D-(17a)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one oxime
  申请人：Tuba Zoltan

  公开号：US20050032763A1

  公开（公告）日：2005-02-10

  The invention relates to a process for the synthesis of d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-oxime (also known as norelgestromin) via acetylation of d-norgestrel at position 17; oximation of the oxo group at position 3 of the obtained d-(17α)-13-ethyl-17-(acetyloxy)-18,19-dinorpregn-4-ene-20-yn-3-one; and then hydrolyzing the acetyloxy group at position 17 of the obtained d-(17α)-13-ethyl-17-(acetyloxy)-18,19-dinorpregn-4-ene-20-yn-3-oxime derivative, thereby obtaining norelgestromin.

  该发明涉及一种合成d-(17α)-13-乙基-17-羟基-18,19-二诺孕烷-4-烯-20-炔-3-酮肟（也称为诺莫酮）的方法，通过在17位对d-诺鲁孕酮进行乙酰化；在得到的d-(17α)-13-乙基-17-(乙酰氧基)-18,19-二诺孕烷-4-烯-20-炔-3-酮的3位的酮基进行氧化反应；然后水解所得的d-(17α)-13-乙基-17-(乙酰氧基)-18,19-二诺孕烷-4-烯-20-炔-3-酮肟衍生物的17位的乙酰氧基，从而获得诺莫酮。
• Methods and Compositions Facilitating Entry of Compounds Into Cells
  申请人：Arya Dev Priya

  公开号：US20080226605A1

  公开（公告）日：2008-09-18

  Disclosed are methods and compositions for facilitating entry of compounds to cells. In some forms, the compositions comprise one or more aminoglycosides and one or more lipids. The disclosed compositions can also comprise one or more compounds or compositions. It was discovered that the disclosed compositions increase the efficiency of delivery of compounds into cells. The disclosed compositions and methods increase both delivery into cells and the activity of compounds once delivered into cells. For example, the disclosed methods and compositions can be used to deliver nucleic acids to cells and to thereby increase the activity of such nucleic acids delivered to cells. The disclosed compositions can be used to deliver compounds and compositions to cells in vitro, ex vivo and in vivo. Delivery can be, for example, non-specific, non-directed, non-targeted, specific, directed or targeted.
• PROCESS FOR THE ENANTIOSELECTIVE ENZYMATIC REDUCTION OF SECODIONE DERIVATIVES
  申请人：Gupta Antje

  公开号：US20110020887A1

  公开（公告）日：2011-01-27

  The invention relates to a process for the enantioselective enzymatic reduction of secodione derivatives. The secodione derivative is reduced with an oxidoreductase/dehydrogenase in the presence of NADH or NADPH as a cofactor. The secodione derivative is used in the reaction batch at a concentration of ≧10 g/l and the oxidized cofactor NAD or NADP formed by the oxidoreductase/dehydrogenase is regenerated continuously.
• US8323936B2
  申请人：——

  公开号：US8323936B2

  公开（公告）日：2012-12-04