http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-071282-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6572ff5df928fd17340eb2a8cb6d8502 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_8e9010f8ae7c32e8b62cd768952bf535 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D281-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D281-10 |
| filingDate | 2009-03-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c889c9ea90b3da80030cebd05c9bcca8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_add096c66ca39d1150e569ab2acf37c0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6e835891e48c90283238a0a0a2c59d07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ca1ee656b7d5fb76dbeff34e7c225014 |
| publicationDate | 2010-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-071282-A1 |
| titleOfInvention | PROCESS TO PREPARE BENZOTIAZEPINS FROM A RANGE - AMINOALQUILBENCENOS |
| abstract | This provides a process for preparing a 2,3,4,5-tetrahydro [1,4] benzothiazepine of formula (1) by the reaction of a [2- (acylaminoethyl) thio] arene of formula (2) with an aldehyde or a multimer of this, and with an acid. The present also provides for the first reaction the [2- (acylaminoethyl) thio] arene with the aldehyde or multimer thereof and a base to form a [N-hydroxymethyl-2- [acylaminoethyl) thio] arene of formula (3), The [N-hydroxymethyl-2- [acylaminoethyl) thio] arene is then treated with the acid to form 2,3,4,5-tetrahydro [1.4] benzothiazepine. Claim 1: A process for preparing a 2,3,4,5-tetrahydro [1,4] benzothiazepine of formula (1) comprising reacting a [2- (acylaminoethyl) thio] arene of formula (2) with an aldehyde of formula R4CHO or a multimer thereof, and with an acid, wherein: Ar is a monocyclic, bicyclic or tricyclic aryl or heteroaryl ring system; R1, R2 and R4 are each, independently, H, C1-20 hydrocarbon, C1-6 alkyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, C1-6-aryl alkyl, C1-6-alkylcycloalkyl, C1- alkyl 6-heterocyclyl or C1-6 alkyl-heteroaryl, each of aryl, cycloalkyl, heterocyclyl and heteroaryl optionally substituted with one to three substituents selected, independently, from the group consisting of halogen, alkyl, alkoxy, nitro, cyano and haloalkyl ; R3 is C1-10 acyl, P (O) R8R9, C (= O) -R10, C (= S) -R11, S (= O) 2R12, (CH2) mR13, a nitrogen protecting group, OH, alkyl C 1-6, cycloalkyl, aryl, heterocyclyl, heteroaryl, C 1-6 alkyl-aryl, C 1-6 alkyl-cycloalkyl, C 1-6 alkyl-heterocyclyl or C 1-6 alkyl-heteroaryl, each of the aryl, cycloalkyl, heterocyclyl and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of halogen, alkyl, alkoxy, nitro, cyano and haloalkyl; or, taken together, R2 and R3 form an oxo-substituted nitrogen containing heterocycle; R5 is, independently, in each of its occurrences H, C1-20 hydrocarbon, C1-6 alkyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, C1-6-aryl alkyl, C1-6-cycloalkyl, C1- alkyl 6-heterocyclyl or C1-6 alkyl-heteroaryl, halogen, acyl, SO3, -OR6, -SR6, -NR6aR6b, -N (R6) C (= O) OR7, N (R6) C (= O) R7, - C (= O) NR6aR6b, -C (= O) OR6, -OC (= O) R6, -NO2, -CN, C1-6 haloalkyl, -O-C1-6 haloalkyl, -N3 or -P (O) R8R9, each of the aryl, cycloalkyl, heterocyclyl and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of halogen, alkyl, alkoxy, nitro, cyano and haloalkyl; R10 and R11 are each, independently, H, -OR14, -NR6aR6b, NHNHR15, NHOH, CONH2NHR15, CO2R15, CONR15, halogen, alkoxy, aryloxy, allyloxy, benzyloxy, substituted benzyloxy, fluoroenylmethoxy, adamantyloxy, C1-hydrocarbon , C 1-6 alkyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, C 1-6 alkyl-aryl, C 1-6 alkyl-cycloalkyl, C 1-6 alkyl-heterocyclyl or C 1-6 alkyl-heteroaryl, each of the aryl, cycloalkyl, heterocyclyl and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of halogen, alkyl, alkoxy, nitro, cyano and haloalkyl; R6, R6a, R6b, R7, R8, R9, R12, R14, R15, R16 and R17 are each, independently, in each of their occurrences, H, -OR15, -NR15R16, NHNHR16, NHOH, C1 hydrocarbon -20, C 1-6 alkyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, C 1-6 alkyl-aryl, C 1-6 alkyl-cycloalkyl, C 1-6 alkyl-heterocyclyl or C 1-6 alkyl-heteroaryl, each of the aryl, cycloalkyl, heterocyclyl and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of halogen, alkyl, alkoxy, nitro, cyano and haloalkyl, or R6a and R6b together with the nitrogen to which they are attached, represent a 5, 6 or 7 membered nitrogen containing heterocycle; R13 is NH2, OH, -SO2R16, -NHSO2R16, C (= O) R17, NH (C = O) R17, -O (C = O) R17 or -P (O) R8R9; m is an integer from 1-10; and q is zero or an integer from 1-4, with the proviso that, when R5 is -C (= O) R6, R5 is not in an ortho position with respect to the sulfur side chain. |
| priorityDate | 2008-03-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 30.