Technique for artificially synthesizing antigen of Sildenafil and derivative thereof

A sildenafil, synthetic technology, applied in the direction of animal/human protein, serum albumin, depsipeptide, etc., can solve the problems of long reaction time, inconvenience, and high experimental cost.

Inactive Publication Date: 2010-12-15
江苏省南通药品检验所
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Problems solved by technology

At present, sildenafil is illegally added to many domestic Chinese patent medicines or health products to achieve clinical efficacy. As a patient, taking Chinese patent medicines or health products containing sildenafil without knowing for a long time will cause serious side effects , When testing whether th

Method used

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  • Technique for artificially synthesizing antigen of Sildenafil and derivative thereof
  • Technique for artificially synthesizing antigen of Sildenafil and derivative thereof
  • Technique for artificially synthesizing antigen of Sildenafil and derivative thereof

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Experimental program
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specific Embodiment approach

[0023] A. Generate water-soluble carbodiimide (EDC):

[0024] Design and synthesize the carboxylic acid derivative of sildenafil (Viagra), its chemical structure is as follows:

[0025]

[0026] Another carboxylic acid derivative of sildenafil (Viagra), its chemical structure is as follows:

[0027]

[0028] Sildenafil generates the reaction formula containing the carboxylic acid derivative of sildenafil as follows:

[0029]

[0030] The specific steps are as follows: (1), alkylation: add 20ml dry dimethylformamide (DMF) and 1.708g, 3.6×10 -3 mol of Nafil-like raw materials or Lafei-like raw materials, and pass N 2 protection, stirred at room temperature, and after dimethylformamide (DMF) was completely dissolved, quickly weighed 0.173g, 4.32×10 -3 mol, concentration is 60% sodium hydride (NaH), and it is added in the described reaction bottle, stirs 50-70 minute, until the solution produces without bubble, draws 1.202g, 7.2 * 10 with 1ml syringe then -3 mol of et...

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Abstract

The invention discloses a technique for artificially synthesizing antigen of Sildenafil and derivative thereof, which comprises the following steps: generating water-soluble EDC, balancing EDC, NHS, DMF and hapten compound to room temperature, weighting EDC, NHS and hapten compound, adding the weighted sample into a clean round bottomed flask, adding DMF, dissolving and marking the generated solution as No.2 reaction solution, dissolving carrier protein in boric acid buffer solution with a ratio of 1:0.15 to 0.2 in another clean container, turning into another clean round bottomed flask and marking the solution as No.3 reaction solution, adding the No.2 reaction solution into the No.3 reaction solution, dialyzing the samples after finishing reaction, cooling and drying the samples into white flocculent products, namely the artificially synthesized antigen.

Description

Technical field: [0001] The invention relates to a technology for artificially synthesizing antigens of sildenafil and derivatives thereof. Background technique: [0002] Sildenafil (Sildenafil), also translated as sildenafil, is a drug for the treatment of male erectile dysfunction that was accidentally invented when developing drugs for the treatment of cardiovascular diseases. The registered name Wei Ergang) is widely known. However, compared with the product name Sildenafil, the common name "Viagra" in China is more widely used and has a greater impact. At present, sildenafil is illegally added to many domestic Chinese patent medicines or health products to achieve clinical efficacy. As a patient, taking Chinese patent medicines or health products containing sildenafil without knowing for a long time will cause serious side effects , When testing whether there are Viagra ingredients in Chinese patent medicines or health care products, the traditional testing method is ...

Claims

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Application Information

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IPC IPC(8): C07K14/795C07K14/765
Inventor 吴迪宏
Owner 江苏省南通药品检验所
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