Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3?-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4?]bipyridinyl-2?-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided.

Abstract: The invention comprises a process for the preparation of a chiral triol of formula I wherein, R1 is hydrogen or halogen by way of an asymmetric hydrogenation of a ketone compound of formula IIa wherein, R1 is hydrogen or halogen and R2 is C1-6-alkyl; with hydrogen in the presence of an iridium spiro-pyridylamidophosphine catalyst (Ir-SpiroPAP catalyst). The chiral triols of formula I are versatile building blocks for the preparation of various pharmaceutically active drug substances such as for instance for statins.

Abstract: The invention relates to a novel process for the preparation of a chiral piperazine-2- carboxylic acid or of a salt thereof of the formula (I). The chiral piperazine-2-carboxylic acid derivatives of the formula (I) are key intermediates for the preparation of fused heteroaryl dihydro pyrimidines which are useful for the treatment and prophylaxis of hepatitis B virus infections.

Abstract: The invention relates to a new process for the preparation of high water affinity type products with controlled humidity via spray drying in a suitable spray drying equipment applying specific spray drying parameters:

Abstract: The invention comprises a process for the preparation of a GalNAc phosphoramidite epimer of the formula (I), wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20, corresponding enantiomers and/or optical isomers thereof and the use of the process for the preparation of GalNAc-cluster oligonucleotide conjugates.

Abstract: The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.

Abstract: The invention comprises LNA-dicarboxylic acid derivatives of the formula I or salts thereof, wherein R1 is a nucleobase or a modified nucleobase R2 is a hydroxy protecting group and n is an integer from 1 to 5. The LNA-dicarboxylic acid derivatives of the formula I can be used in preloaded solid supports of the formula III and as that serve as suitable start material for oligonucleotide synthesis.

Abstract: The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.

Abstract: The invention relates to a process for the preparation of a compound of formula (I) or a salt thereof.

Abstract: The invention relates to compounds of the formula and to a process for making same and to the use of the products in the solid phase peptide synthesis. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.

Abstract: The invention relates to compounds of the formula and to a process for making same and to the use of the products in the solid phase peptide synthesis. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.

Abstract: Provided herein is a process for the preparation of oxytocin receptor agonists that have the potential to be used for the treatment of neurological disorders.

Abstract: The invention relates to compounds of the formula and to a process for making same and to the use of the products in the solid phase peptide synthesis. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.

Abstract: The invention relates to compounds of the formula I. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.

Abstract: A novel process for the preparation of imidazo[1,2-a]pyridine compounds of the formula wherein R1 is C1-4-alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen or C1-4-alkyl or R4 and R5, together with the nitrogen atom to which they are attached, form a saturated 4- to 6-membered heterocyclic ring which may contain one further heteroatom selected from nitrogen or oxygen; R2 is C1-4-alkyl, C1-4-alkoxycarbonyl, halogen, phenyl which is optionally substituted with C1-4-alkyl, C1-4-alkoxy or halogen or is NR4R5 wherein R4 and R5 are independently hydrogen or C1-4-alkyl or R4 and R5, together with the nitrogen atom to which they are attached, form a saturated 4- to 6-membered heterocyclic ring which may contain one further heteroatom selected from nitrogen or oxygen; R3 is C1-4-alkyl and X is nitrogen or CH is described.

Abstract: A novel process for the preparation of imidazo[1,2-a]pyridine compounds of the formula wherein R1 is C1-4-alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen or C1-4-alkyl or R4 and R5, together with the nitrogen atom to which they are attached, form a saturated 4- to 6-membered heterocyclic ring which may contain one further heteroatom selected from nitrogen or oxygen; R2 is C1-4-alkyl, C1-4-alkoxycarbonyl, halogen, phenyl which is optionally substituted with C1-4-alkyl, C1-4-alkoxy or halogen or is NR4R5 wherein R4 and R5 are independently hydrogen or C1-4-alkyl or R4 and R5, together with the nitrogen atom to which they are attached, form a saturated 4- to 6-membered heterocyclic ring which may contain one further heteroatom selected from nitrogen or oxygen; R3 is C1-4-alkyl and X is nitrogen or CH is described.

Abstract: The invention relates to a novel process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I or of a salt thereof wherein R1 stands for hydrogen, a halogen, for an optionally protected hydroxyl group or for an optionally protected amino group and R2 is hydrogen or a halogen. 2-Phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I with their 1,2,4-triazole nucleus build the structural core of a great number of functionalized molecules in medicinal chemistry.

Abstract: The invention relates to compounds of the formula to a process for making same and to the use of the products in the solid phase peptide synthesis. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.

Abstract: The invention relates to a process for the preparation of a compound of formula (I) or a salt thereof.

Abstract: The invention relates to a novel process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I or of a salt thereof wherein R1 stands for hydrogen, a halogen, for an optionally protected hydroxyl group or for an optionally protected amino group and R2 is hydrogen or a halogen. 2-Phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I with their 1,2,4-triazole nucleus build the structural core of a great number of functionalized molecules in medicinal chemistry.