A method for preparing (dimethylaminomethylene) malononitrile by using a micro reaction system. Cyanoacetamide, N,N-dimethylformamide and a catalyst are mixed to obtain a mixture, and the mixture and phosphorus oxychloride are simultaneously pumped into the micro reaction system that includes a micromixer and a microchannel reactor connected in series for continuous dehydration condensation. After adjusted to a target pH, the crude product is subjected to continuous liquid-liquid extraction with an organic solvent in a centrifugal extraction unit comprising a plurality of annular centrifugal extractors connected in series. The organic phase is collected to obtain the target product (dimethyl aminomethylene) malononitrile.

A method for preparing (dimethylaminomethylene) malononitrile by using a micro reaction system. Cyanoacetamide, N,N-dimethylformamide and a catalyst are mixed to obtain a mixture, and the mixture and phosphorus oxychloride are simultaneously pumped into the micro reaction system that includes a micromixer and a microchannel reactor connected in series for continuous dehydration condensation. After adjusted to a target pH, the crude product is subjected to continuous liquid-liquid extraction with an organic solvent in a centrifugal extraction unit comprising a plurality of annular centrifugal extractors connected in series. The organic phase is collected to obtain the target product (dimethyl aminomethylene) malononitrile.

Reaction pathways and conditions for the production of nitrogen-containing chelators, such as a glycine derivative, with reduction of ammonia byproducts. In particular, the present disclosure describes a process for the production of a nitrile intermediate by reacting a tetra-amino compound or dinitrile compound with an aldehyde and a hydrogen cyanide to form the nitrile intermediate. The nitrile intermediate may then be further processed to produce chelators at a high yield and/or a high purity.

Reaction pathways and conditions for the production of nitrogen-containing chelators, such as a glycine derivative, with reduction of ammonia byproducts. In particular, the present disclosure describes a process for the production of a nitrile intermediate by reacting a tetra-amino compound or dinitrile compound with an aldehyde and a hydrogen cyanide to form the nitrile intermediate. The nitrile intermediate may then be further processed to produce chelators at a high yield and/or a high purity.

A process for making a complexing agent with an enantiomeric excess of at least 60%, wherein said process comprises the following steps: (a) reacting an aqueous slurry of alanine with an enantiomeric excess of at least 60% with formaldehyde and hydrocyanic acid, thereby forming an aqueous solution of alanine-bisacetonitrile, (b) saponifying the alanine-bisacetonitrile from step (a) by combining the aqueous solution obtained in step (a) with an aqueous solution of alkali metal hydroxide.

A process for making a complexing agent with an enantiomeric excess of at least 60%, wherein said process comprises the following steps: (a) reacting an aqueous slurry of alanine with an enantiomeric excess of at least 60% with formaldehyde and hydrocyanic acid, thereby forming an aqueous solution of alanine-bisacetonitrile, (b) saponifying the alanine-bisacetonitrile from step (a) by combining the aqueous solution obtained in step (a) with an aqueous solution of alkali metal hydroxide.

The present invention relates to alanine N-acetic acid precursors of formula (i) COOM-CH(CH3)-NH—(CH2CN), wherein M is hydrogen (alanine N-monoacetonitrile), or (ii) COOM-CH(CH3)-N—(CH2CN)2, wherein 0 to 50% of all M is sodium or potassium and 50 to 100% of all M is hydrogen (alanine N,N-diacetonitrile and its partial sodium or potassium salts) comprising L-alanine to D-alanine in a range of from 75:25 to 50:50 (L:D), or (iii) COOM-CH(CH3)-N—(CH2CONH2)2, wherein M is hydrogen (alanine N,N-diacetamide), in the form of crystals, and relates to a process to prepare these precursors and their use, especially to give MGMA or MGDA.

The present invention relates to alanine N-acetic acid precursors of formula (i) COOM-CH(CH3)-NH—(CH2CN), wherein M is hydrogen (alanine N-monoacetonitrile), or (ii) COOM-CH(CH3)-N—(CH2CN)2, wherein 0 to 50% of all M is sodium or potassium and 50 to 100% of all M is hydrogen (alanine N,N-diacetonitrile and its partial sodium or potassium salts) comprising L-alanine to D-alanine in a range of from 75:25 to 50:50 (L:D), or (iii) COOM-CH(CH3)-N—(CH2CONH2)2, wherein M is hydrogen (alanine N,N-diacetamide), in the form of crystals, and relates to a process to prepare these precursors and their use, especially to give MGMA or MGDA.

The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.

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The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.

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