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UNIBIOCHEM

Amino acid derivatives

Both solid phase peptide synthesis and solution phase peptide synthesis are demanding a growing array of protected amino acids. These peptide syntheses require amine protection, side-chain protection, and often acid activation or protection. The addition order of the protecting groups can have a significant influence on both the cost and quality of a particular derivative. UNIBIOCHEM has extensive experience in kilos-to-tons manufacturing of this wide array of protected amino acids.

Alpha-Amine Protection	Side-Chain Protection	Carboxyl Protection
Acetyl-	Benzyl-	Benzyl-
Boc-	tert-Butyl-	Cyclohexyl ester-
Cbz-	Trityl-	Ethyl-
Fmoc-	Tosyl-	Methyl-
Trityl-	Nitro-	tert-Butyl-
etc...	etc...	etc...

Non-natural amino acids and derivatives continue to gain importance in drug development. Reliable, cost-effective commercial supply of these intermediates is crucial for a successful drug launch. Unibiochem employs the most cost-effective manufacturing processes to provide high-quality Non-natural amino acids on an industrial scale.

Unibiochem have developed expertise in both enzymatic and chemical routes to specialty amino acids. The acylase route is a well-established, cost-effective process for producing both enantiomers of many specialty amino acids. Hydantoinase enzymes can be used to provide high yields of high-purity D form amino acids. Other enzymes, including transaminase and nitrilase, are also evaluated in select situations. Non-enzymatic (chemical) processes, including asymmetric hydrogenation, chiral auxiliary and classical resolution methods, are also employed by Unibiochem.

Peptides

UNIBIOCHEM has developed expertise in the solution phase manufacture of small peptides, the ultimate products most often derived from amino acids. The choices of protection group, activating group, order of addition and coupling agent lead to numerous alternate potential peptide synthesis routes. Our experience in the manufacture of the protected amino acids as well as solution phase coupling allows us to quickly target the most cost effective process. UNIBIOCHEM's efficient production of amino acid derivatives provides the critical raw materials for peptide fragments, which we have manufactured by solution phase on a metric ton scale.

Our partner has equipped with solid phase peptide synthesis instruments such as high-pressure liquid chromatograph and analytical apparatus and so on, enabling us to offer peptide raw materials and peptide pharmaceuticals from gram base to kilogram base.

Advanced intermediates

Unibiochem takes its unnatural amino acids "downstream" to the manufacture of many complex chiral intermediates. Multiple adjacent chiral centers, required for an increasing number of developmental drugs, can be accessed through amino acid derivative chemistry. The chemistry required for these derivatives, including hydrogenation, Grignard and hydride additions, condensations reactions and others, has been practiced on a multi-ton scale at Unibiochem. Most of this chemistry is carried out under confidentiality protocol.

Acetylation	Acylation	Alkylation	Amidation
Ammonolysis	Bromination	Chlorination	Condensation
Coupling reaction	Cyanation	Decarboxylation	Dehydration
Dehydrogenation	Diazotization	Elimination	Esterification
Friedel-Crafts reaction	Grignard reaction	Halogenation	Hydrogenation
Nitration	Nitrosation	Oxidation	Ozonization reaction
Thiophosgene	Phosgenation

Custom synthesis (Development and manufacturing)

· Group protection (especially for amino acids)

· Solution phase peptide synthesis

· Catalytic hydrogenation (Raney-Ni, Pd-Carbon)

· Halogenation reactions (Fluoro-, Chloro-, Bromo- and Iodo-)

· Hazardous reactions (Phosgenation, SOCl2, HCN etc.)

· Organometallic reactions (Organo-Lithium, Sodium etc.)

· Reaction pressures ranges from 0.1mmHg to 100 bar

· Reaction temperatures ranges from -80°C to 300°C

IP Protection:

IP Protection is deemed as top strategic priority for the long-term development of our company.

An NDA (Non Disclosure Agreement) is signed by all the employees.

Only those authorized scientists & visits are allowed to enter the lab and photography is prohibited without prior permission.

Control of information: A code name is assigned to each project, electronic communication, usage of computers are closely monitored and duplication or copy of documents has strict regulations.

Procedures to minimize risk: Laboratory notebook is scanned regularly and electronic information is backuped frequently for disaster recovery.