Pharmaceutical intermediate refers to intermediate compounds used in the pharmaceutical process to synthesize drugs. They are key intermediate products that are gradually synthesized into drugs through a series of organic synthesis reactions, starting from raw materials or natural products. Pharmaceutical intermediates play an important role in drug development and production. They are one of the key steps in converting molecules with therapeutic activity into final drugs. By controlling the synthesis route of intermediates and optimizing reaction conditions, efficient and sustainable drug production can be achieved.
Intermediate can provide customers with a complete set of services including the development of pharmaceutical intermediate production processes, optimization of commercial production, and registration and declaration. Following the regulations and guidelines of ICH and NMPA, we also provide customized synthesis services for high-end pharmaceutical intermediates with stable quality, controllability, cost-effectiveness, and high product added value for drug research and development enterprises, manufacturers, outsourcing service providers, and scientific research institutions.
There are many types of pharmaceutical intermediates, and the following are some common pharmaceutical intermediates:
Benzene ring intermediates: It refers to intermediate products or molecules formed in chemical reactions that contain a benzene ring structure. The benzene ring is a cyclic structure formed by six carbon atoms, which has stability and special electronic properties. It is widely present in organic compounds and many natural products, and plays an important role in synthesizing new compounds, constructing organic frameworks, and adjusting molecular properties.
Here are some common benzene ring intermediates:
l Phenol: Phenol is a compound containing a benzene ring and a hydroxyl group (- OH). It can be formed by replacing the hydrogen on the benzene ring with a hydroxyl group. Phenol and its derivatives have important applications in the pharmaceutical, dye, and chemical industries.
l Aniline: Aniline is a compound containing a benzene ring and an amino group (- NH2). It can be formed by replacing the hydrogen on the benzene ring with an amino group. Aniline and its derivatives have a wide range of applications in the dye, pharmaceutical, and rubber industries.
Phenylboronic acid intermediate: 7-Methyl-1,3-dihydro-2,1-Benzoxazoro-1-ol
Pyridine intermediates: It refers to intermediate products or molecules formed in chemical reactions that contain pyridine ring structures. Pyridine is a six membered heterocyclic ring composed of five carbon atoms and one nitrogen atom. It has stability and unique electronic properties, making these intermediates very valuable in constructing complex molecular skeletons, introducing specific functional groups, and regulating molecular properties, and can be applied in the fields of organic synthesis and drug development. Pyridine itself is also an important compound, commonly used as a solvent and a component of many drugs and natural products.
Here are some common pyridine intermediates:
l Aminopyridine: It is an organic compound with a pyridine ring and an amino group. It is a derivative of pyridine, with an amino substituent on the pyridine ring in its structure. In drug research, aminopyridine and its derivatives play an important role. For example, 4-aminopyridine is used as a drug to treat multiple sclerosis and myasthenia gravis, which can improve muscle control and alleviate symptoms by increasing nerve conduction velocity.
l Niacinamide: Niacinamide is a compound containing a pyridine ring and an amide group. It is a form of vitamin B3 widely used in the pharmaceutical and health product industries.
l Pyridinecarboxylic acid: Pyridine ketone is a type of compound containing a pyridine ring and a carbonyl (ketone or acid) group. It can be formed by replacing the hydrogen atom on pyridine with a carbonyl group. Pyrinone compounds are commonly used as intermediates in organic synthesis and drug development, and can undergo various chemical reactions.
Aminopyridine: Ethyl 4-amino-6-chloro-5-iodopyridine-3-carboxylate
Deuterated intermediates refer to intermediate products or molecules formed in chemical reactions that contain deuterium (deuterium substituted hydrogen). Deuterium is an isotope of hydrogen, which contains one proton and one neutron in its nucleus, and is heavier than the proton of ordinary hydrogen. Deuterated intermediates can be used in the fields of organic synthesis and drug development to study reaction mechanisms, alter chemical properties, and perform nuclear magnetic resonance analysis.
The following are common deuterated intermediates:
l Deuterated anisole: It refers to the compound obtained by replacing the hydrogen atom in anisole with deuterium atom. Benzyl ether is an aromatic compound whose molecular structure consists of a benzene ring and a methoxy (- OCH3) group. Deuterated benzyl ether has certain application value in organic chemistry research. Due to the isotopic effects between deuterium (D) and hydrogen (H), which can sometimes cause differences in chemical properties, replacing hydrogen atoms with deuterium atoms can provide different reaction kinetics and product selectivity under specific experimental conditions. Deuterated benzyl ether can be used to study reaction mechanisms, investigate ion exchange processes, and perform nuclear magnetic resonance (NMR) analysis.
l Deuterated solvent: In the laboratory, deuterated solvents such as deuterated chloroform (CDCl3), deuterated dimethyl sulfoxide (DMSO-d6), deuterated methanol (CD3OD), etc. are commonly used as reaction media. Deuterated solvents can be used for solvent displacement reactions in the synthesis process, as well as for the determination of NMR spectra, providing rich information.
Deuterated spirocyclic intermediate: 6-Azaspiro [2.5] Octane-1,1-D2
Pyrimidine intermediates are a common organic compound with a six membered heterocyclic structure composed of four carbon atoms and two nitrogen atoms. Pyrimidine plays an important biological role in organisms, for example, among the five bases that form DNA and RNA, three are derivatives of pyrimidine: Cytosine, Thymine, and Uracil. Pyrimidine intermediates are intermediate products generated during pyrimidine synthesis or reaction. Pyrimidine has a wide range of applications, especially playing an important role in drug development and organic synthesis. Here are several common pyrimidine intermediates:
l Cytosine: It is a pyrimidine base and amino pyrimidine has important biological functions in organisms. It participates in the synthesis of DNA and RNA and plays an important role in the transmission of genetic information in cells. In the field of pharmaceuticals, aminopyrimidines and their derivatives are also widely used. For example, anti metabolic drugs such as 5-aminopyrimidine can be used to treat diseases such as leukemia and kidney disease.
l Halogenated Pyrimidine: It refers to compounds that undergo halogen substitution on pyrimidine molecules. Common halogenated pyrimidines include Chlorouracil, Bromouracil, Iodouracil, etc. Halopyrimidine has chemical properties similar to pyrimidine, and also exhibits special properties in some biological activities and pharmaceutical applications. For example, in anti-tumor therapy research, certain halogenated pyrimidines have anti-tumor activity. For example, fluorouracil (5-FU) is a commonly used anti-cancer drug, which is widely used to treat a variety of cancers, such as colon cancer, gastric cancer and breast cancer. Fluorouracil can prevent the growth and proliferation of tumor cells by interfering with cellular metabolic processes.
Intermediate of halogenated pyrimidine: 5-bromo-2-ethylpyrimidine
Heterocyclic intermediates refer to cyclic molecules formed in chemical reactions that contain at least one non carbon atom (usually nitrogen, oxygen, sulfur, etc.). In organic synthesis, it helps to construct complex molecular skeletons and introduce specific functional groups, thereby achieving the synthesis and adjustment of target compounds. At the same time, these heterocyclic compounds also have a wide range of biological activities and potential applications, which are of great significance for research in pharmaceuticals and other chemical fields.
Here are some common heterocyclic intermediates:
l Thiophene: Thiophene is a five membered heterocyclic ring composed of four carbon atoms and one sulfur atom. Due to its structural stability and electronic properties, thiophene and its derivatives have important applications in anticancer drugs.
l Pyrrole: Pyrrole is a five membered heterocyclic ring composed of four carbon atoms and one nitrogen atom. Some pyrrole compounds also have biological activity, such as the pyrrole structure in hemoglobin.
l Imidazole: Imidazole is a five membered heterocyclic ring composed of three carbon atoms and two nitrogen atoms. Imidazole and its derivatives are widely used in drug development as antifungal drugs, penetrating agents, and metal coordination reagents.
Benzimidazole intermediates: 3- (4-bromo-3-methyl-2-oxo-2,3-dihydro-1H-benzo [D] imidazol-1-yl) piperidine-2,6-dione
Pharmaceutical intermediates play a crucial role in drug synthesis, enabling the effective and controlled synthesis of bioactive compounds with the necessary characteristics for therapeutic applications. In the research and development of protac drugs, Intermediate provides the design and synthesis of the target protein PROTAC-POI, summarizes popular POI ligands, E3ligase ligands of different tissue types, and establishes a linker library containing hundreds of linker molecules. In terms of nucleic acid drug research and development, the Intemedi nucleotide drug chemical synthesis platform can provide one-stop monomer synthesis and modification; Oligonucleotide synthesis; Synthesis of delivery systems and oligonucleotide conjugates. The siRNA library we have built not only has a rich inventory of monomers, but also a huge library of monomer synthesis blocks, which can quickly complete the synthesis of various modified monomers.
At the same time, there are multiple chemical ADC payload molecules with different mechanisms of action available in the compound library of Intermediate for customers to choose from, and one or several ADC anti-tumor chemical drugs can be customized and synthesized according to the specific needs of customers. The ADC payloads molecular library of Intermediate can effectively solve the problem of selecting cell toxins. In the ADC payloads molecular library, the Intermediate drug discovery team has accumulated a variety of different mechanisms of action and types of cell toxins for customers to choose from. At the same time, one or several ADC cell toxins that customers need can be customized and synthesized to meet their quantity requirements. Through independent research and external cooperation, InteMedi can provide 6 toxins of all ADC drugs already on the market, and can synthesize self-developed toxins by providing more than 20 derivatives of toxins in ADC drugs already on the market.
