153438-48-3

Upstream product

• 624-92-0 Dimethyldisulphide 
• 4623-24-9 2-(3-aminophenyl)acetonitrile 
• 6011-14-9 2-aminoacetonitrile hydrochloride 
• 128312-11-8 3-methylthiophenylboronic acid 
• 59083-33-9 (3-methylsulfanyl-phenyl)-methanol 
• 90555-55-8 1-chloromethyl-3-methylsulfanylbenzene 
• 151-50-8 potassium cyanide 

Downstream Products

• 372938-32-4 [(3-methylsulfanyl-phenyl)ethyl]carbamic acid tert-butyl ester 
• 118468-20-5 2-(3-methylsulfanyl-phenyl)ethylamine 

Relevant academic research and scientific papers

Synthesis of α-aryl esters and nitriles: Deaminative coupling of α-aminoesters and α-aminoacetonitriles with arylboronic acids

Transition-metal-free synthesis of α-aryl esters and nitriles using arylboronic acids with α-aminoesters and α-aminoacetonitriles, respectively, as the starting materials has been developed. The reaction represents a rare case of converting C(sp3)-N bonds into C(sp3)-C(sp2) bonds. The reaction conditions are mild, demonstrate good functional-group tolerance, and can be scaled up. Touch base: A transition-metal-free protocol for the synthesis of α-aryl esters and nitriles by deaminative coupling is presented. Strong bases and transition-metal catalysts are not needed. The new synthetic method uses readily available starting materials and demonstrates wide substrate scope.

Benzoxazines for use in the treatment of parkinson's disease

Benzoxazines of Formula (I) wherein R1 is C1-C6 alkyl, C2-C6 alkenyl, or (CH2)n phenyl, R2 is C3-C6 alkyl, R3 is hydrogen, halo, hydro

Synthesis and pharmacology of benzoxazines as highly selective antagonists at M4 muscarinic receptors

Previously, we reported on PD 102807 (41) as being the most selective synthetic M4 muscarinic antagonist identified to date. Synthesized analogues of 41 showed no improvement in affinity and selectivity at that time. However, several newly synthesized compounds exhibit a 7-fold higher affinity at M4 receptors and demonstrate a selectivity of at least 100-fold over all other muscarinic receptor subtypes. For example, compound 28 showed an affinity of pKi = 9.00 at M4 receptors and a selectivity of M1/M4 13 183-fold, M2/M4 = 339-fold, M3/M4 = 151-fold, and M5/M4 = 11 220-fold. This high selectivity along with high affinity has not been reported for any synthetic muscarinic antagonist, nor for natural occurring M4 antagonists such as the M4 selective Eastern Green Mamba venom MT3 (M4 pKb = 8.7, M1/M4 = 40-fold, M2/M4 ≥ 500-fold, M3/M4 500-fold, and M5/M4 ≥ 500-fold). Derivative 24, a compound with a high selectivity pattern as well, has been tested for in vivo efficacy. It was able to block the L-3,4-dihydroxyphenylalanine accumulation produced by CI-1017, an M1/M4 selective muscarinic agonist, in the mesolimbic region and striatum, which suggests that 24 is capable of crossing the blood-brain barrier and confirms the pharmacokinetic data obtained on this compound. This is evidence that suggests that agonist-induced increase in catecholamine synthesis observed in these regions is mediated by M4 receptors.

Herbicidal pyridopyridazinones and pyridopyridazinethiones

Pyrido[2,3-d]pyridazin-5-one and pyrido[2,3-d]pyridazin-5-thione derivatives of general formula (I): STR1 wherein R and R1 independently represent hydrogen, optionally halogenated alkyl, alkenyl or alkynyl, optionally substituted heterocycle or a group --[CR41 R42 ]n -(phenyl)-(R3)q ; R2 represents halogen, optionally halogenated alkyl, alkenyl or alkynyl, CN; --CO2 R4 ; --S(O)r R4 ; --NO2 ; --NR41 R42 ; --OH; --COR4, --S(O)r R5, --CO2 R5, --OR5 ; --CONR41 R42, --OSO2 R5, --OSO2 R6, --OCH2 R5, --N(R41)COR6, --N(R41)SO2 R5, --N(R41)SO2 R6, --SO2 NR41 R42, optionally substituted phenyl, alkoxy or haloalkoxy; X represents oxygen or sulphur; R3 represents halogen, optionally halogenated alkyl, alkenyl, alkoxy, alkynyl, --OH, --S(O)r R4, --CO2 R4, COR4, --CN, --NO2, --NR41 R42, --OR5 ; --CONR41 R42, --OSO2 R5, --OSO2 R6, --OCH2 R5, --N(R41)COR6, --N(R41)SO2 R5, --N(R41)SO2 R6 or --SO2 NR41 R42 ; R4 represents a hydrogen atom or optionally halogenated C1-6 alkyl; R41 and R42, which may be the same or different, each represents a hydrogen atom or optionally halogenated C1-4 alkyl; R5 represents a phenyl group optionally substituted by from one to five groups selected from halogen, nitro, cyano, R4 and --OR4 ; m represents zero or an integer from one to three; n represents zero, one or two; where n is two, the groups --(CR41 R42)-- may be the same or different; q represents zero or an integer from one to five; r represents zero, one or two; with the proviso that when m represents zero R and R1 do not simultaneously represent hydrogen; and agriculturally acceptable salts thereof are useful as herbicides.