HAPILA Chemical Synthesis

HAPILA GmbH offers its customers a range of practical solutions for development and cGMP production of sophisticated drug substances.

Development as well as manufacturing services include chemical synthesis, purification and particle design.

In chemical synthesis, HAPILA offers a range of multistage processes to synthesize highly active pharmaceutical ingredients (HAPIs) including creation of the required analytical and stability data, reports and documents required for regulatory compliance.

HAPILA also focuses on optimization of existing processes as well as testing and realization of alternative synthesis routes.

Chemical Synthesis Services

HAPILA offers a range of relevant chemical synthesis services. These include:

• developing new synthesis processes for manufacture of active pharmaceutical ingredients (APIs) and Intermediates
• innovative synthesis design for new substances as well as for those already available on the market
• generating feasibility studies on innovative synthesis approaches based on intensive investigations in literature and patents
• optimization of synthesis routes, with development of alternatives where necessary
• handling of highly active substances
• scale-up of synthesis processes up to 100L scale in-house
• process transfer to external production plants.

Classes of Substances

HAPILA has experiences in the handling and processing of the full range of substance classes involved in synthesizing HAPIs. These include:

• steroidanalogues
• aminoacids
• flavones
• porphins
• benzothiazinones

Reactions

The chemical synthesis of HAPIs and highly potent active pharmaceutical ingredients (HPAPIs) involve a wide range of potential chemical reactions. HAPILA has the facilities and capabilities to undertake any of the following:

• Regioselective and stereoselective reduction and (ep)oxidation
• Bromination and chlorination
• Cross-coupling reactions
• McMurry homo-coupling reaction
• Gabriel synthesis of primary amines
• Nitration
• Simmons-Smith cyclopropanation
• Shapiro reaction
• Silylations and de-silylations
• Esterifications or amidations
• Acidic and alkaline hydrolysis
• Ethinylation
• Carboxylations
• Birchreduction
• Grignard reactions
• Catalytic hydrogenation.

cGMP synthesis

All HAPILA chemical syntheses are carried out at in-house in its GMP certified laboratories at Gera, Thuringia, in east-central Germany.

When combined with purification and particle design, HAPILA’s chemical synthesis services cover the complete API value-creation chain, enabling it to be a highly efficient bridge-builder between API production and pharmaceutical end-use.