41035-30-7

Upstream product

• 58-00-4 apomorphin 
• 18605-42-0 10,11-dimethoxy-6-methyl-aporphane 
• 76-57-3 codeine 
• 38291-33-7 (R)-10,11-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline 
• 641-36-1 Apocodeine 
• 18605-43-1 10,11-dimethoxy-6-methyl-5,6-dihydro-4H-dibenzo[de,g]quinoline 
• 57-27-2 MORPHIN 
• 467-14-1 Neopin 
• 86680-39-9 3-O-acetyl-6-O-mesylneomorphine 
• 86680-37-7 3-O-acetylneomorphine 
• 86709-01-5 neomorphine 
• 86545-92-8 demethoxyoripavine 
• 120-14-9 3,4-dimethoxy-benzaldehyde 
• 2033-89-8 3,4-dimethoxyphenol 

Downstream Products

• 1334547-61-3 8-[2-(methylamino)-ethyl]-phenanthrene-3,4-dioxide 
• 18605-40-8 oxoapomorphine 
• 58534-36-4 (R)-MDO-Apomorphine 
• 58-00-4 5,6,6a,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol 
• 42337-29-1 Di-isobutyryl-apomorphin 

Relevant academic research and scientific papers

PHARMACEUTICAL COMPOSITION FOR USE IN THE TREATMENT OF NEUROLOGICAL DISEASES

The present invention relates to pharmaceutical compositions for administration to mammals that include (6aS)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient that provides pharmacokinetic profiles useful for the treatment of neurodegenerative diseases.

PRODUCTION PROCESS OF A HYDROCHLORIC ACID SALT OF APOMORPHINE AND DERIVATIVES THEREOF

The present invention provides processes for the preparation of a hydrochloric acid salt of compound of formula (2): (I) Compound of formula (2) wherein: R1 is selected from the group consisting of -H, an unsubstiuted straight-chain C1-C20-alkyl, substituted straight-chain C1-C20-alkyl, unsubstituted branched -chain C1-C20-alkyl, substituted branched-chain C1-C20-alkyl, unsubstituted cyclic C3-C20-alkyl, and substituted cyclic C3-C20-alkyl; and R2 is selected from the group consisting of an unsubstituted straight-chain C1-C20-alkyl, substituted straight-chain C1-C20-alkyl, unsubstituted branched-chain C1-C20-alkyl, substituted branched-chain C1-C20-alkyl, unsubstituted cyclic C3-C20-alkyl, substituted cyclic C3-C20-alkyl, unsubstituted -C1-20-alkyl-C3-20-cycloalkyl, substituted -C1-20-alkyl-C3-20-cycloalkyl, unsubstituted allyl and substituted allyl.

PHARMACEUTICAL COMPOSITIONS OF (6AS)-6-METHYL-5,6,6A,7-TETRAHYDRO-4H-DIBENZO[DE,G]QUINOLINE-10,11-DIOL

This invention relates to pharmaceutical compositions for enhancing the solubility of (6aS)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol and salt forms thereof.

Convergent Total Synthesis of (±)-Apomorphine via Benzyne Chemistry: Insights into the Mechanisms Involved in the Key Step

Convergent total synthesis of (±)-apomorphine hydrochloride was accomplished by an approach that employs in the key step a sequence of transformations involving a [4+2]-cycloaddition reaction followed by a hydrogen migration. Through this sequence of transformations, the desired aporphine core was obtained regioselectively in 75% isolated yield. Since only one regioisomer was produced in the key step of the synthesis, a polar [4+2]-cycloaddition mechanism was proposed. Furthermore, NMR experiments and theoretical calculations were carried out to elucidate the hydrogen migration mechanism. (±)-Apomorphine hydrochloride was achieved after 9 steps in an overall yield of 8% involving benzyne chemistry.

FACILE 'ONE POT' PROCESS FOR APOMORPHINE FROM CODEINE

An improved method for producing apomorphine and derivatives thereof is provided. The method is a convenient 'one-pot' process, comprising the conversion of codeine into apomorphine without isolating the apocodeine intermediate. Use of water reactive scavengers, reagents that will react irreversibly with water, decreases side product formation and allows the use of milder reaction conditions. This one-pot synthesis of apomorphine from codeine provides a faster reaction with improved yields at temperatures lower as compared to conventional methods. The lower operating temperatures and less volatile reactants make the method particularly useful for large-scale manufacturing.