N-(苯基磺酰基)-D-丝氨酸 | 103197-51-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: N-(苯基磺酰基)-D-丝氨酸
• 英文名称: N-(Phenylsulfonyl)-D-serine
• 英文别名: N-phenylsulfonyl-D-serine；(R)-2-benzenesulfonylamino-3-hydroxy-propionic acid；N-benzenesulfonyl-D-serine；(2R)-2-(benzenesulfonamido)-3-hydroxypropanoic acid
• CAS: 103197-51-9
• 化学式: C₉H₁₁NO₅S
• 分子量: 245.256
• InChiKey: WQVIJBXPLXLSCI-MRVPVSSYSA-N

物化性质

• 熔点：
  232-233 °C (decomp)
• 沸点：
  491.4±55.0 °C(Predicted)
• 密度：
  1.481±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  112
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  N-(苯基磺酰基)-D-丝氨酸 在 正丁基锂 、 硼烷四氢呋喃络合物 、 L-Selectride 、 对甲苯磺酸 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 77.17h， 生成 (4R,5R)-4-(3-Hydroxypropyl)-2,2-dimethyl-5-<(phenylsulfonyl)amino>-1,3-dioxane
  参考文献：
  名称：

  Synthesis of Carbacephems from Serine

  摘要：

  Carbacephems have been synthesized from D-serine by two routes involving construction first of the six-membered ring followed by cyclization to give the bicyclic beta-lactam. In one route, alkylation of a lactim ether was accomplished with Ni(Acac)(2) as a catalyst. The desired R stereochemistry at the carbon corresponding to C-6 of the cephem was obtained by stereospecific hydrogenation of a vinylogous carbamate. The second route involved a stereospecific Michael cyclization to give the same C-6 stereochemistry. Closure of a piperidyl beta-amino acid intermediate common to both routes was accomplished using a modified Mukaiyama reagent found to be superior in our system to the traditional reagent. The resulting carbacephem core was stereospecifically substituted at C-7 with an ethyl or amino functionality. The ethylated intermediate was transformed into a stable enol triflate useful for the further elaboration of biologically important carbacephems.

  DOI：

  10.1021/jo980592s
• 作为产物：
  描述：

  D-丝氨酸 、 苯磺酰氯 以to give (R)-2-benzenesulfonylamino-3-hydroxy-propionic acid的产率得到N-(苯基磺酰基)-D-丝氨酸
  参考文献：
  名称：

  IMIDAZOLIDINONE DERIVATIVES

  摘要：

  这项发明涉及公式(I)的新型咪唑啉酮衍生物，其中R1到R11和X如描述和权利要求中所定义，并且其生理上可接受的盐。这些化合物与LXR alpha和LXR beta结合，可用于制备药物组合物。

  公开号：

  US20080242677A1

文献信息

• PARAKERATOSIS INHIBITOR, PORE-SHRINKING AGENT OR AGENT FOR PREVENTING/AMELIORATING ROUGH SKIN AND EXTERNAL COMPOSITION FOR SKIN
  申请人：Shiseido Company, Limited

  公开号：EP1884230A1

  公开（公告）日：2008-02-06

  The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin -inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and to further provide an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor agent, pore-shrinking agent, or rough skin preventing/amaliorating agent comprises one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof. The external composition for skin comprises the one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent.

  该发明提供了一种具有角化不全抑制、收缩毛孔或防止/改善粗糙皮肤功能的抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂，不会引起感觉刺激等安全问题，非常安全，并进一步提供了一种外用皮肤组合物，其中添加了具有上述功能的化合物。角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂包括从α-氨基酸衍生物和其盐组成的群中选择的一种、两种或更多化合物。外用皮肤组合物包括从α-氨基酸衍生物和其盐组成的群中选择的一种、两种或更多化合物，作为上述角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂。
• Parakeratosis inhibitor, pore-shrinking agent,or rough skin preventing/ameliorating agent, and external composition for skin
  申请人：Kaminuma Mikiko

  公开号：US20090215893A1

  公开（公告）日：2009-08-27

  The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin-inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and to further provide an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor agent, pore-shrinking agent, or rough skin preventing/amaliorating agent comprises one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof. The external composition for skin comprises the one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent.

  本发明提供了一种角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂，具有角化不全抑制、毛孔收缩或防止/减轻粗糙皮肤等功能，不会引起感觉刺激等安全问题，非常安全，进一步提供了一种添加了具有上述功能的化合物的皮肤外用组合物。该角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂包含从α-氨基酸衍生物和其盐的组中选择的一种、两种或更多化合物。该皮肤外用组合物包含从α-氨基酸衍生物和其盐的组中选择的一种、两种或更多化合物，作为上述角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂。
• Imidazolidinone derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US07625902B2

  公开（公告）日：2009-12-01

  The invention is concerned with novel imidazolidinone derivatives of formula (I): wherein R1 to R11 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used in pharmaceutical compositions.

  本发明涉及式(I)的新型咪唑啉酮衍生物，其中R1至R11和X在说明书和权利要求书中定义，以及其生理上可接受的盐。这些化合物与LXR alpha和LXR beta结合，可用于制备药物组合物。
• WRINKLE-PREVENTIVE/AMELIORATING AGENT
  申请人：SHISEIDO COMPANY, LTD.

  公开号：EP1908454A1

  公开（公告）日：2008-04-09

  A wrinkle-preventing and -improving composition comprising one or more than one compound selected from the group consisting of α-amino acid derivatives represented by the following general formula (1) and salts thereof: wherein, R1 represents hydrogen atom, CH3 group or CH2OH group, R2 and R3 each independently represent hydrogen atom, alkyl group having 1 to 4 carbons, provided that R2 and R3 cannot be hydrogen atom at the same time, or R2 and R3 together with N atom to which they are bound may form a ring structure having a total carbon number of 4 to 6, in which case said ring structure may optionally contain an oxygen atom as a heteroatom, R4 represents hydrogen atom, alkyl group having 1 to 18 carbons, wherein when R1 and R4 are hydrogen atom, it cannot be that one of R2 and R3 is benzyloxycarbonyl group and the other is hydrogen atom.

  一种防皱和改善皱纹的组合物，包含一种或一种以上选自下式（1）所代表的 α-氨基酸衍生物及其盐类的化合物： 其中，R1 代表氢原子、CH3 基团或 CH2OH 基团，R2 和 R3 各自独立地代表氢原子、具有 1 至 4 个碳原子的烷基，但 R2 和 R3 不能同时为氢原子，或者 R2 和 R3 与它们所结合的 N 原子可形成一个总碳数为 4 至 6 的环结构、R4 代表氢原子或碳原子数为 1 至 18 的烷基，其中当 R1 和 R4 为氢原子时，R2 和 R3 不能一个为苄氧羰基，另一个为氢原子。
• INHIBITORS OF UROKINASE AND BLOOD VESSEL FORMATION
  申请人：CORVAS INTERNATIONAL, INC.

  公开号：EP1100814A2

  公开（公告）日：2001-05-23