Gemcitabine, chemically known as 2′,2′ -difluoro-2 ‘-deoxycytidine, is an important antitumor drug precursor and a very important pharmaceutical intermediate. The following is an overview of its properties, preparation and application:
Nature:
Gemcitabine is a water-soluble pyrimidine nucleotide analogue with a structure that includes a deoxysugar molecule and a pyrimidine base (cytosine), and is replaced by two fluorine atoms at the 2′ position, which gives it good antitumor activity.
As a white or white-like crystalline solid, gemcitabine is unstable under physiological conditions, so it is usually provided in the form of a hydrochloride, gemcitabine hydrochloride, when used clinically.
Preparation:
The synthesis of gemcitabine is a complex process involving several steps, including site-specific fluoridation of intermediates and the introduction and removal of protective groups.
In industrial production, a common strategy is to synthesize a stable and industrially viable hydroxyl protectant intermediate through a series of chemical reactions, which are then converted into the final gemcitabine product.
Applications:
– Anti-tumor therapy: Gemcitabine is mainly used in the treatment of a variety of solid tumors, such as pancreatic cancer, non-small cell lung cancer, bladder cancer, breast cancer and ovarian cancer.
– Mechanism of action: After entering the cell, gemcitabine can be phosphorylated into an active nucleotide and incorporated into the DNA strand that is replicating, thereby preventing tumor cell proliferation by inhibiting ribonucleotide reductase during DNA synthesis and repair.
– Combination therapy: Gemcitabine can be used alone or in combination with other chemotherapy agents (such as 5-FU, cisplatin, etc.) or other therapies (such as radiotherapy) to enhance treatment effectiveness and overcome single-drug resistance.
Please note that the actual preparation method is subject to patent protection and technical confidentiality, and the specific application is determined according to the doctor’s prescription and the specific situation of the patient.
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Wisdom Drugs Co .,Ltd was founded in Sep. 2011 whose headquarter located in Changzhou Creative Industry Park, having a branch in India. The company’s R&D center is engaged in not only the process development of APIs, intermediates, poly-peptide compounds and heterocyclic compounds,but also the optimization and production. We are devoted to the synthesis customization and the technology transfer, enabling compounds to be scaled from laboratory to commercial to meet the requirements of different customers.
