tetramethylguanidinium azide

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: tetramethylguanidinium azide
• 英文别名: (N,N-dimethylcarbamimidoyl)-dimethylazanium;azide
• 化学式: C₅H₁₄N₃*N₃
• 分子量: 158.206
• InChiKey: ZMMRLWFGWQVVJD-UHFFFAOYSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  0.0
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  35.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (4R)-3-[(2R,3S)-2-bromo-3-(4-bromophenyl)butanoyl]-4-phenyl-1,3-oxazolidin-2-one 、 tetramethylguanidinium azide 在 crude product 、 hexanes ethyl acetate 作用下， 以 乙腈 为溶剂， 反应 12.0h， 生成 (4R)-3-[(2S,3S)-2-azido-3-(4-bromophenyl)butanoyl]-4-phenyl-1,3-oxazolidin-2-one
  参考文献：
  名称：

  Cyclohexylalanine derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes

  摘要：

  本发明涉及一种新型的环己基丙氨酸衍生物，其是二肽基肽酶-IV酶（“DP-IV抑制剂”）的抑制剂，并且在治疗或预防二肽基肽酶-IV酶参与的疾病，例如糖尿病和特别是2型糖尿病方面有用。本发明还涉及包含这些化合物的制药组合物以及在预防或治疗二肽基肽酶-IV酶参与的这种疾病中使用这些化合物和组合物。

  公开号：

  US07671073B2

文献信息

• Cephalosporins having an imino substituted piperazindioncarbonylamino
  申请人：E. R. Squibb & Sons, Inc.

  公开号：US04386199A1

  公开（公告）日：1983-05-31

  Cephalosporins of the formula ##STR1## wherein R is hydrogen, sodium, potassium, or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl, furyl, or pyridyl, or 2-amino-4-thiazolyl; R.sub.3 is lower alkyl or substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl, or furyl; R.sub.4 is hydrogen or lower alkyl; and X is hydrogen, ##STR2## --O--lower alkyl, or certain substituted or unsubstituted heterothio groups; are disclosed. These compounds possess useful antibacterial activity.

  本发明揭示了式为##STR1##的头孢菌素，其中R为氢、钠、钾或某些酯基；R.sub.1在α-构型中为氢或甲氧基；R.sub.2为氢、低碳基、环烷基、环烯基、环烷二烯基、取代或未取代的苯基、苄基、苯乙基、噻吩基、呋喃基或吡啶基，或2-氨基-4-噻唑基；R.sub.3为低碳基或取代或未取代的苯基、苄基、苯乙基、噻吩基或呋喃基；R.sub.4为氢或低碳基；X为氢、##STR2## --O--低碳基，或某些取代或未取代的杂硫杂环基团。这些化合物具有有用的抗菌活性。
• Penicillins having an imino substituted piperazindioncarbonylamino acyl
  申请人：E. R. Squibb & Sons, Inc.

  公开号：US04189482A1

  公开（公告）日：1980-02-19

  Penicillins of the formula ##STR1## wherein R is hydrogen , sodium, potassium or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, lower aklkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl, furyl, or pyridyl, or 2-amino-4-thiazolyl; R.sub.3 is lower alkyl or substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl or furyl; and R.sub.4 is hydrogen or lower alkyl; are disclosed. These compounds possess useful antibacterial activity.

  公式为##STR1##的青霉素，其中R为氢，钠，钾或某些酯基; R.sub.1处于α构型，为氢或甲氧基; R.sub.2为氢，较低的烷基，环烷基，环烯基，环烷二烯基，取代或未取代的苯基，苄基，苯乙基，噻吩基，呋喃基或吡啶基，或2-氨基-4-噻唑基; R.sub.3为较低的烷基或取代或未取代的苯基，苄基，苯乙基，噻吩基或呋喃基; R.sub.4为氢或较低的烷基; 这些化合物具有有用的抗菌活性。
• .beta.-Lactam antibiotics, their preparation and use
  申请人：Beecham Group Limited

  公开号：US04413000A1

  公开（公告）日：1983-11-01

  The present invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sup.3 is a hydrogen atom or is an organic bonded via a carbon atom to the carbapenem ring, n is zero or one, X is a saturated or unsaturated hydrocarbon radical optionally substituted by bromo or chloro, and R.sup.4 is a C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-10 aralkyl or aryl group, any of such groups R.sup.4 being optionally substituted. These compounds are useful as antibacterial agents.

  本发明提供了式（II）的化合物：##STR1##及其盐和酯，其中R.sup.3是氢原子或通过碳原子与卡那霉素环结合的有机基团，n为零或一，X是饱和或不饱和的碳氢基团，可选地被溴或氯取代，R.sup.4是C.sub.1-6烷基，C.sub.2-6烯基，C.sub.1-10芳基烷基或芳基基团，其中任何这样的基团R.sup.4均可选择性地被取代。这些化合物可用作抗菌剂。
• Antibacterial 3-(5-tetrazolyl) penam compounds
  申请人：Pfizer Inc.

  公开号：US04179511A1

  公开（公告）日：1979-12-18

  Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.

  某些新型6-酰胺基-2,2-二甲基-3-(5-四唑基)青霉烷衍生物及其盐；它们作为广谱抗菌剂的用途，以及它们的制备方法。它们的制备包括对新型中间体6-氨基-2,2-二甲基-3-(5-四唑基)青霉烷或其简单衍生物进行酰化，然后在某些情况下，通过进一步转化6-酰胺基团或从5-四唑基部分去除保护基。制备6-氨基-2,2-二甲基-3-(5-四唑基)青霉烷、其简单衍生物及其中间体的方法。
• Process for production of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam and
  申请人：Pfizer Inc.

  公开号：US03994939A1

  公开（公告）日：1976-11-30

  A chemical process which comprises reacting 6-(2-phenylacetamido)- or 6-(2-phenoxyacetamido)-2,2-dimethyl-3-(5-tetrazolyl)penams and certain derivatives thereof which carry a blocking or pseudo blocking group on the tetrazolyl moiety with a halogenating agent at or below 0.degree. C. to form the corresponding imino halide, followed by reaction of the imino halide with an alcohol below about -20.degree. C. to form the corresponding imino ether, and hydrolyzing the imino ether under acid conditions. The preparation of the starting 6-acyl-2,2-dimethyl-3-(5-tetrazolyl)penams is described.

  一种化学过程，包括将带有阻断或伪阻断基团的6-(2-苯乙酰胺基)-或6-(2-苯氧乙酰胺基)-2,2-二甲基-3-(5-四唑基)青霉烷及其衍生物与卤化试剂在0℃以下反应，形成相应的亚胺卤化物，然后在-20℃以下的醇中反应，形成相应的亚胺醚，并在酸性条件下水解亚胺醚。还描述了起始6-酰基-2,2-二甲基-3-(5-四唑基)青霉烷的制备过程。