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850649-62-6 Alogliptin Benzoate C25H27N5O4 691-730-4 Antidiabetic

850649-62-6 Alogliptin Benzoate C25H27N5O4 691-730-4 Antidiabetic

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    Antidiabetic Pharmaceutical Intermediates

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    850649-62-6 Alogliptin Benzoate

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    C25H27N5O4 Alogliptin Benzoate

  • Product Name
    Alogliptin Benzoate
  • Synonyms
    ALOGLIPTIN(SYK-322) BENZOATE;(R)-2-((6-(3-Aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benz;2-[[6-[(3R)-3-aMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-Benzonitrile Monobenzoate
  • CAS
    850649-62-6
  • MF
    C25H27N5O4
  • MW
    461.52
  • EINECS
    691-730-4
  • Purity
    99%
  • Place of Origin
    China
  • Brand Name
    RUN
  • Certification
    IOS9001
  • Model Number
    RUN-Z
  • Minimum Order Quantity
    10g
  • Price
    inquiry
  • Packaging Details
    10g 50g 100g 500g 1kg
  • Delivery Time
    3-7 days
  • Payment Terms
    T/T, MoneyGram, BTCcoin
  • Supply Ability
    1kg --100kg

850649-62-6 Alogliptin Benzoate C25H27N5O4 691-730-4 Antidiabetic

SECTION 1: Basic information

Alogliptin benzoate Basic information
Indications and Usage Mechanisms of Action Adverse reactions
Product Name: Alogliptin benzoate
Synonyms: (R)-2-((6-(3-aMinopiperidin-1-yl)-3-Methyl-2,4-dioxo-3,4-dihydropyriMidin-1(2H)-yl)Methyl)benzonitrile benzoate;Alogliptin benzoate 2-[[6-[(3R)-3-Amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile benzoate;Alogliptin(Alogliptin benzoate;2-[6-[3(R)-AMinopiperidin-1-yl]-3-Methyl-2,4-dioxo-1,2,3,4-tetrahydropyriMidin-1-ylMethyl]benzonitrile benzoate Monobenzoate;Alogliptin API;ALOGLIPTIN(SYK-322) BENZOATE;(R)-2-((6-(3-Aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benz;2-[[6-[(3R)-3-aMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-Benzonitrile Monobenzoate
CAS: 850649-62-6
MF: C25H27N5O4
MW: 461.52
EINECS: 691-730-4
Product Categories: antidiabetic;Inhibitors;Final material;pharmaceutical intermediate;API
Mol File: 850649-62-6.mol
Alogliptin benzoate Structure
 
Alogliptin benzoate Chemical Properties
 
Safety Information
MSDS Information
 
 
Alogliptin benzoate Usage And Synthesis
Indications and Usage Alogliptin (benzoic acid) is a type-2 diabetes medication, and it is a type of serine protease dipeptidyl peptidase IV (DPP-4) inhibitor developed by the Japanese company Takeda. Alogliptin, used alone or in combination with other blood sugar-lowering medication, is usually well-tolerated in type-2 diabetes patients. This medication has a low risk of hypoglycemia, with Alogliptin treatment groups ≤8.3% and placebo groups ≤10.5%, and shows no difference between young and elderly patients. In addition to effectively lowering blood sugar, this medicine also lowers the risks of hypoglycemia and weight increase, overcoming great obstacles in patient treatment and providing new hope for diabetes treatment.
Mechanisms of Action Alogliptin selectively inhibits DPP-4 to reduce the inactivation of glucagon-like peptide 1 (GLP-1) and increase the GLP-1 levels in the body, thus lowering blood sugar. Once blood sugar reaches normal levels, it will cease its sugar-lowering effects, thus effectively reducing the risks of hypoglycemia. Additionally, DPP-4 inhibitor also slows gastric emptying, increases the feeling of fullness, and controls appetite, thus helping patients control their weight.
Adverse reactions Common side effects of Alogliptin include nasopharyngitis, headaches, and upper respiratory tract infection. Most side effects are light to moderate and are unrelated to dosage.
Uses Treatment of type 2 diabetes.
Definition ChEBI: A benzoate salt obtained by combining equimolar amounts of alogliptin and benzoic acid. Used for treatment of type 2 diabetes.
Clinical Use Alogliptin benzoate is a dipeptidyl peptidase IV (DPPIV) inhibitor discovered by Takeda Pharmaceuticals and approved in Japan in 2010 for the treatment of type II diabetes mellitus. Alogliptin is an oral drug for once a day dosing to complement diet and exercise. Alogliptin is the most selective marketed DPPIV inhibition and has similar PK and PD properties compared to previous entries. The discovery, structure-activity relationship of related analogs, and synthesis of this compound have been recently published.
Chemical Synthesis The most convenient synthesis for scale-up will be highlighted from several published routes. Commercially available 2-cycanobenzyl amine 1 was reacted with methylisocyanate in DCM at ambient temperature to provide N-methyl urea 2 in 85% yield. Reaction of the urea 2 with dimethyl malonate in refluxing ethanol with sodium ethoxide as base gave the cyclized trione 3 in 78-85% yield. The trione 3 was then refluxed in neat POCl3 to provide the penultimate chloride crude 4 in 95% yield which was reacted with Boc-protected diamine 5 in the presense of potassium carbonate in DMF to furnish alogliptin I in 93-96% yield. Treatment of alogliptin with benzoic acid in ethanol at 60-70 °C followed by crystallization delivered the desired alogliptin benzoate (I).

850649-62-6 Alogliptin Benzoate C25H27N5O4 691-730-4 Antidiabetic 1

 

SECTION 2: Hazard identification

2.1 Classification of the substance or mixture

Not classified.

2.2 GHS label elements, including precautionary statements

Pictogram(s) No symbol.
Signal word No signal word
Hazard statement(s) none
Precautionary statement(s)
Prevention none
Response none
Storage none
Disposal none

2.3 Other hazards which do not result in classification

no data available

SECTION 3: Composition/information on ingredients

3.1 Substances

Chemical name Common names and synonyms CAS number EC number Concentration
2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl] benzonitrile;benzoic acid 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl] benzonitrile;benzoic acid 850649-62-6 691-730-4 100%

SECTION 4: First-aid measures

4.1 Description of necessary first-aid measures

If inhaled

Move the victim into fresh air. If breathing is difficult, give oxygen. If not breathing, give artificial respiration and consult a doctor immediately. Do not use mouth to mouth resuscitation if the victim ingested or inhaled the chemical.

Following skin contact

Take off contaminated clothing immediately. Wash off with soap and plenty of water. Consult a doctor.

Following eye contact

Rinse with pure water for at least 15 minutes. Consult a doctor.

Following ingestion

Rinse mouth with water. Do not induce vomiting. Never give anything by mouth to an unconscious person. Call a doctor or Poison Control Center immediately.

4.2 Most important symptoms/effects, acute and delayed

no data available

4.3 Indication of immediate medical attention and special treatment needed, if necessary

no data available

SECTION 5: Fire-fighting measures

5.1 Suitable extinguishing media

Use dry chemical, carbon dioxide or alcohol-resistant foam.

5.2 Specific hazards arising from the chemical

no data available

5.3 Special protective actions for fire-fighters

Wear self-contained breathing apparatus for firefighting if necessary.

SECTION 6: Accidental release measures

6.1 Personal precautions, protective equipment and emergency procedures

Avoid dust formation. Avoid breathing mist, gas or vapours.Avoid contacting with skin and eye. Use personal protective equipment.Wear chemical impermeable gloves. Ensure adequate ventilation.Remove all sources of ignition. Evacuate personnel to safe areas.Keep people away from and upwind of spill/leak.

6.2 Environmental precautions

Prevent further spillage or leakage if it is safe to do so. Do not let the chemical enter drains. Discharge into the environment must be avoided.

6.3 Methods and materials for containment and cleaning up

Collect and arrange disposal. Keep the chemical in suitable and closed containers for disposal. Remove all sources of ignition. Use spark-proof tools and explosion-proof equipment. Adhered or collected material should be promptly disposed of, in accordance with appropriate laws and regulations.

SECTION 7: Handling and storage

7.1 Precautions for safe handling

Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.

7.2 Conditions for safe storage, including any incompatibilities

Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.

SECTION 8: Exposure controls/personal protection

8.1 Control parameters

Occupational Exposure limit values

no data available

Biological limit values

no data available

8.2 Appropriate engineering controls

Ensure adequate ventilation. Handle in accordance with good industrial hygiene and safety practice. Set up emergency exits and the risk-elimination area.

8.3 Individual protection measures, such as personal protective equipment (PPE)

Eye/face protection

Wear tightly fitting safety goggles with side-shields conforming to EN 166(EU) or NIOSH (US).

Skin protection

Wear fire/flame resistant and impervious clothing. Handle with gloves. Gloves must be inspected prior to use. Wash and dry hands. The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it.

Respiratory protection

If the exposure limits are exceeded, irritation or other symptoms are experienced, use a full-face respirator.

Thermal hazards

no data available