The present invention provides processes for the preparation of Dasotraline (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for the production of the compound of Formula (2), or a salt thereof, and its deprotection to afford Dasotraline (1).

##STR00001##

The present invention provides processes for the preparation of Dasotraline (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for the production of the compound of Formula (2), or a salt thereof, and its deprotection to afford Dasotraline (1).

##STR00001##

The present invention provides processes for the preparation of Dasotraline (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for the production of the compound of Formula (2), or a salt thereof, and its deprotection to afford Dasotraline (1).

##STR00001##

A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.

A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.

A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.

Disclosed in the present invention is a method for preparing a tertiary amine by using a secondary amine as a raw material. The method comprises a step of reacting a secondary amine that serves as a raw material with an acid to generate a proton-type ionic liquid, and a step of reacting the proton-type ionic liquid with an aldehyde under the action of a reducing agent to generate a tertiary amine. The secondary amine is an aliphatic secondary amine and/or an aromatic secondary amine and/or a cyclic secondary amine; the acid is selected from one of or a combination of several of an organic carboxylic acid and an inorganic acid; the aldehyde is a monoaldehyde, a dialdehyde or an aldehyde polymer; and the reducing agent is selected from one of or a combination of several of formic acid, sodium formate, oxalic acid, sodium oxalate and triphenylsilane.

Disclosed in the present invention is a method for preparing a tertiary amine by using a secondary amine as a raw material. The method comprises a step of reacting a secondary amine that serves as a raw material with an acid to generate a proton-type ionic liquid, and a step of reacting the proton-type ionic liquid with an aldehyde under the action of a reducing agent to generate a tertiary amine. The secondary amine is an aliphatic secondary amine and/or an aromatic secondary amine and/or a cyclic secondary amine; the acid is selected from one of or a combination of several of an organic carboxylic acid and an inorganic acid; the aldehyde is a monoaldehyde, a dialdehyde or an aldehyde polymer; and the reducing agent is selected from one of or a combination of several of formic acid, sodium formate, oxalic acid, sodium oxalate and triphenylsilane.

Disclosed in the present invention is a method for preparing a tertiary amine by using a secondary amine as a raw material. The method comprises a step of reacting a secondary amine that serves as a raw material with an acid to generate a proton-type ionic liquid, and a step of reacting the proton-type ionic liquid with an aldehyde under the action of a reducing agent to generate a tertiary amine. The secondary amine is an aliphatic secondary amine and/or an aromatic secondary amine and/or a cyclic secondary amine; the acid is selected from one of or a combination of several of an organic carboxylic acid and an inorganic acid; the aldehyde is a monoaldehyde, a dialdehyde or an aldehyde polymer; and the reducing agent is selected from one of or a combination of several of formic acid, sodium formate, oxalic acid, sodium oxalate and triphenylsilane.

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. ##STR00001##